FORM 2THE PATENTS ACT 1970 (39 of 1970) & The Patent Rules 2003COMPLETE SPECIFICATION (see sections 10 & rule 13)
1. TITLE OF THE INVENTIONAntifungal CompoundsAnd Process Thereof
2. APPLICANT (S)
NAME NATIONALITY ADDRESS

FDC Ltd INDIAN B-8 MIDC Industrial Estate ,Waluj -431136, Maharashtra
CSIR INDIAN Anusandhan Bhavan, Rafi Marg, New Delhi 110 001
3. PREAMBLE TO THE DESCRIPTION
CompleteThe following specification particularly describes the invent! it is to be performed. on and the manner in which

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Antifungal Compounds And Process Thereof
Field of Invention:
The present invention relates to compounds of formula (1), its solvates and
pharmaceutically acceptable salts having antifungal activity. The invention also relates to
a process for the preparation of said compounds and its pharmaceutical composition
comprising an effective amount of compound of formula (I).
F
Formula(l)
Wherein R = Me and the remaining radicals R1 and R2 each independently of others hydrogen or halogen or carboxyl or alkyl carboxyl or carboxyester or alkyl carboxyester or alhyl cyono or 1-(1, 2,4 triazolyll), its solvates and its salts of such compounds having at least one salt forming group
.Wherein R = H, and the remaining radicals R1 and R2 each independently of others hydrogen or halogen or carboxyl or alkyl carboxyl or carboxyester or alkyl carboxyester or alkyl cyano or 1 -(1,2,4 triazolyl) or represent CI -C4 alkyl, C.3 -C.6 cycloalkyl, CI -C4 haloalkyl, CI -C.4 alkoxy, CI -C4 haloalkoxy, halogen, nitro, cyano, hydroxy, benzyloxy, hydroxymethyl, NR, -CONR, CH.2 --OCO--R., CO--R4, --SO.,-CNHR, 1-pyrrolyl, 1-imidazolyl, lH-l,2,4-triazol-l-yl, 5-tetrazolyl, 1-pyrrolidinyl, 4-morpholinyl, 4-morpholinyl-N-oxide.

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Background of the Invention:
Azole based antifungal agents are known in the literature being used for the treatment of fungal infection. However, with growing fungal infections and emergence of pathogens resistant to some of the antifungal drugs already existing in the market, as an urgent need for broad spectrum antifungal agent which are effective against certain mycoses (such as aspergillosis) for which no effective treatment is available.
In the past decades the frequency and types of life-threatening fungal infection have increased dramatically in immuno-compromised patients. Several factors have contributed to rise such as the expansion of severely ill and or immuno-compromised patient populations with HIV infection, with chemotherapy induced neutropenia, and receiving immunosuppressive therapy; more invasive medical procedures, such as extensive surgery and the use of prosthetic devices and vascular catheters; treatment with broad-spectrum antibiotics or glucocorticosteroids; and peritoneal dialysis or hemodialysis.
This problem of increased fungal infections is accentuated by the emergence of fungal strains which are resistant to currently used antifungal agents. Mojor opportunistic fungal pathogens include Candida albicans, Aspergillus, Fusurian spp. Other species of Candida such as C, krusei, C tropicalis, C.glabrata are major causative agents of candidiasis. Invasive pulmonary aspergillosis is a leading cause of mortality in bone marrow transplant recipients. HIV-infected patients are particularly susceptible to mucosal candidiasis, cryptcoccal meningitis.
Fluconazol is the preferred broad spectrum anti-fungal agent used in treatment of fungal infections. In recent times resistance of Candida albicans the most common cause of mucosal candidiasis in HIV-infected patients, after long-term suppressive therapy, to azoles, particularly fluconazole, is a cause of increasing concern. Resistance to fluconazole in other Candida species and in Cryptococcus neoformans has also been reported. Also, fluconazoleappears to be less active against the two emerging Candida

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species, C. glabratta and C. krusei. Infection with Aspergillus, although not common, is frequently life-threatening, and fluconazole has only moderate activity against this fungi.
This has necessitated the need for new antifungal agents with broad spectrum of antifungal activity, which this invention seeks to provide.
Prior Art of the Invention.
US Patent No.5,807,854 describes antifungal agents which covers generically compounds of formula (I) of the present invention wherein R = Me
rYF 2
y
F
Formula (I)

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Objects of the Invention:
Primary object of the invention is to provide compounds of formula (I)as an antifungal agent.
An object of the invention is to provide an antifungal agent having broader spectrum of activity.
Another object of the invention is to provide a process for the preparation of antifungal compound of formula (I).
Yet another object of the invention is to provide a pharmaceutical composition comprising an effective amount of antifungal compound of formula (I).
Still another object of the invention is to provide solvate or pharmaceutical acceptable salts of compounds of formula (I).
Summary of the Invention:
The present invention relates to antifungal compounds represented by general formula (I), its solvate or pharmaceutically acceptable salts and its pharmaceutical composition. The invention also relates to a process for the preparation of compounds of formula (I) .In the process of preparation of compounds of formula (I) the compounds may also be obtained as its solvates or pharmaceutically acceptable salts.

6
Description of Table:
Table refers to the antifungal activity results
Detailed Description of Invention:
In accordance with the object, the present invention provides compound of formula (I), its solvates or pharmaceutically acceptable salts.
/Ns OH? WVR1
V
F Formula (I)
Wherein R = Me and the remaining radicals R1 and R2 each independently of others hydrogen or halogen or carboxyl or alkyl carboxyl or carboxyester or alkyl carboxyester or alhyl cyono or 1-(1,2,4 triazolyl), its solvates and its salts of such compounds having at least one salt forming group.
Wherein R = H, and the remaining radicals Ri and R2 each independently of others hydrogen or halogen or carboxyl or alkyl carboxyl or carboxyester or alkyl carboxyester or alkyl cyano or 1 -{1,2,4 triazolyl) or represent CI -C4 alkyl, C.3 -C.6 cycloalkyl, CI -C4 haloalkyl, CI -C.4 alkoxy, CI -C4 haloalkoxy, halogen, nitro, cyano, hydroxy, benzyloxy, hydroxymethyl, NR, -CONR,CH.2 -OCO-R., CO--R4, --SO.,-CNHR, 1-pyrrolyl, 1-imidazolyl, lH-l,2,4-triazolyl, 5-tetrazolyl, 1-pyrrolidinyl, 4-morpholinyl, 4-morpholinyl-N-oxide.

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/Nv OH? WVR1
F In an embodiment of the invention preferred compounds of formula (I) are R = H ,
R1=R2= H, Br and/or I, its solvates and pharmaceutically acceptable salt of such
compounds having at least one salt forming group.
R=Me R1 = R2 = H, Br, I and / or 1 - (1,2,4 - Triazolyl), its solvates and pharmaceutically acceptable salt of such compounds having at least one salt forming group
Another embodiment provides pharmaceutical composition comprising a compound of formula (I) or its solvates or pharmaceutically acceptable salts of such compound having at least one salt forming group together with a pharmaceutical carrier.
Yet another embodiment of the invention provides a method for the treatment or prevention of a fungal infection in a substrate, said method comprising administering a compound formula 1 as claimed in claim lor a pharmaceutically acceptable salt of such compound having at least one salt forming group or solvate thereof to a substrate in need of such treatment or prevention.
Still another embodiment provides human being or animal as substrate.
A pharmaceutical composition comprising compound of formula(I) or its solvate or pharmaceutically acceptable salt of such compound having at least one salt forming group for the treatment or prevention of fungal infections
A process for the preparation of compound of formula (I), wherein R=H or its solvate or pharmaceutically acceptable salt of such compound having atleast one salt forming group, said process comprising steps of:
a) contacting oxiranyl compound of formula (2),

Formula (2)
with thienopyrimidone compound of formula(3) in an organic solvent in presence of base and a catalyst

Formula (3)
Wherein R1 and R2 each independently of others defined for R being H as above
b) to obtain compound of formula (1), and

R1
fNwlKr
FX=N R2


Formula (1)
R1 and R2 each independently of others defined for R being H as above
c) converting the compound of formula (1) to its pharmaceutically acceptable salt by adapting conventional method..

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A process for the preparation of compound of formula (I), wherein R=Me or its solvate or pharmaceutically acceptable salt of such compound having atleast one salt forming group, said process comprising steps of:
a) contacting compound of formula (5)

F formula (5)
with thieno pyrimidone compound of formula(3) in an organic solvent in presence of base and a catalyst
W/ R2
Formula (3)
Wherein R1 and R2 each independently of others defined for R being Me as
above
b) to obtain compound of formula (6),

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Formula(6)
Wherein R1 and R2 each independently of others defined for R being Me as above
c) contacting compound (6) of step (b) with trimethylsulfoxinium iodide in an organic solvent containing aqueous base, phase transfer catalyst at a temperature ranging between 10° C to 45°C to obtain compound of formula(7),

Formula (7)
Wherein R1 and R 2 each independently of others defined for R being Me as above
d) contacting compound (7) with 1,2,4-triazole in an organic solvent in presence of a base at a temperature ranging between 0° to 60° C for a time period of 10 to 25 h to yield compound of formula (1), and

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Formula(l)
Wherein R] and R2 each independently of others defined for R being Me as above
e) converting the compound of formula (1) to its pharmaceutically acceptable salt by
adapting conventional method.. A use of a compound of formula (I) or its solvates or a pharmaceutically acceptable solt of said compound having at least one solt forming group for the preparation of a pharmaceutically composition for use in the treatment or prevention of antifungal infections.
A pharmaceutical composition preferably in capsule or tablet form for the treatment or prevention of fungal infection.
A compound of formula(l) along with pharmaceutically acceptable excipients for treatment or prevention of fungal infection in human beings or animals.
The compounds of present invention may be used in agrochemical composition and for prevention and treatment of plant fungal infection.
The compounds of the present invention may be prepared by adapting the route depicted in scheme I or II as herein below:

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Scheme 1




FVrr,/ R2
, base

R1 and R2 each independently of others defined for R being H as above
This invention relates to a process for the preparation of 6 and /or 7 substituted or unsubstituted-3-[2-( difluorophenyl -2-hydroxy-3-( 1,2,4)triazol-1 -ylpropyl]-3H-thieno[3,2-d]pyrimidin-4-ones of the formula (1). More particularly it relates to the process for the preparation of (1) from l[[2-(difluorophenyl)oxiranyl]methyl]-l//-1,2,4-triazole of the formula (2) by reacting with 6 and /or 7 substituted or unsubstituted thieno-[3,2-d]pyrimidine-4(3//)-one of the formula( 3.)
Accordingly the present invention describes a process for the preparation of of 6 and /or 7 substituted or unsubstituted 3-[2-(difluoro-phenyl)-2-hydroxy-3-(l,2,4)triazol-l-ylpropyl]-3//-thieno[3,2-d]pyrimidin-4-ones of the formula (1) wherein, Rl, R2 may be defined as hydrogen, halogen and /or 1,2,4-triazol-l-yl radical, which comprises reacting l[[2-( /difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole of the formula(2) with 6 and /or 7 substituted or unsubstituted -thieno-[3,2-d]pyrimidine-4(3H)-one of the formula (3) in a suitable organic solvent in presence of a suitable base and a PTC catalyst] at temperature 40-90 °C for a suitable period, cooling to ambient temperature, removing the organic solvent, diluting with water, extracting with suitable water immiscible organic solvent, separating the organic layer, washing with water, drying over drying agent, concentrating

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and purifying the product by column chromatography to collect the required compound of the formula (1),[R=H].
Structures of some of preferred oxarinyl and thieno pyrimidone compounds used to obtain preferred compounds of formula(l), wherein R is defined as hydrogen by adapting scheme 1 is depicted below::

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ABSTRACT
The present invention relates to compounds of formula (1), its solvates and pharmaceutically acceptable salts having antifungal activity and its pharmaceutical composition comprising an effective amount of compound of formula (I). The invention also relates to a process for the preparation of said compounds by contacting essentially the required oxiranyl compound and thienopyrimidone compound under appropriate conditions and finally treating optionally with 1,2,4-triazole in presence of a base to obtain some of the preferred compounds of the invention.


f\=H/ R2

Formula (1)

14

3A

3B

3C

1D

S^ A
MY
1A

1B

1C


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Scheme 2

R1 and R2 each independently of others defined for R being Me as above
The present invention describes a process for the preparation of 6and/or7-substituted or unsubstituted )-3 -[2-( difluoro-phenyl)-2-hydroxy-1 -methyl-3 -(1,2,4)triazol-1 -ylpropyl] -3/f-thieno[3,2-d]pyrimidin-4-ones of the formula(l)wherein Rl and R2 may be hydrogen, halogen or 1,2,4-triazol-l-yl radical which comprises reacting 2-halo-l-( difluorophenyl)-1-propanone of the formula (5) with( 6and/or7-substituted or unsubstituted)-thieno-[3,2-d]pyrimidine-4(3//)-one of the formula (3) in a suitable organic solvent in presence of a suitable base and a catalyst at temperature 40-90 °C for a suitable period, cooling to ambient temperature, diluting with water, separating the organic layer, washing with water, drying over drying agent, concentrating, purifying by column chromatography(to collect the intermediate of the formula (6), dissolving the intermediate (6) in a suitable organic solvent, adding it to a mixture of trimethylsulfoxonium iodide, a suitable base, water, phase transfer catalyst and a suitable organic solvent, stirring at temperature 10-45

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°C for a suitable period, cooling to ambient temperature, diluting with water, separating the organic layer, washing with water, drying over drying agent, concentrating, purifying by column chromatography to collect the intermediate of formula( 7), reacting the intermediate(T) with 1,2,4-triazole in presence of base in a suitable organic solvent at 0-60 °C for 12-20 h, removing the organic solvent on rotavapour, diluting with water, extracting with organic solvent, washing with water, drying over drying agent, concentrating and purifying by column chromatography to isolate(6and/or7-substituted orunsubstituted )-3-[2-(difluorophenyl)-2-hydroxy-l-methyl-3-(l,2,4)triazol-l-ylpropyl]-3^-thieno[3,2-d]pyrimidin-4-ones of the formula((l),[R=Me].
Structures of some of the preferred oxarinyl and thieno pyrimidone compounds used to obtain preferred compounds of formula (1), wherein R is defined as Me by adapting scheme 2 is depicted below

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*N 3E
TJO

3B

3D

3A

3C




6A




6C

6D

18

7C

7D

7E




1H

7C

7D

7E




4D


1K

1L

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Accordingly the active compounds of formula (I) of the present invention provides composition that contain a compound of the present invention together with an excipient and optionally other auxiliary agents .The compounds of the present invention can be administered in different pharmaceutical preparations, the nature of which will depend, as it is well known, upon the chosen route of administration and the nature of the pathology to be treated.
Thus, solid compositions according to the present invention for oral administration include compressed tablets, dispersible powders, granules and capsules. In tablets, the active component is admised with at least one inert diluent such as lactose, starch, mannitol, microcrystalline cellulose or calcium phosphate; granulating and disintegrating agents for example corn starch, gelatine, microcrystalline cellulose or polyvinylpyrrolidone; and lubricating agents for example magnesium stearate, stearic acid or talc. The tablets may be coated by known technique to delay disintegration and absorption in the gastrointestinal tract and, thereby, provide a sustained action over a longer period. Gastric film-coated or enteric film-coated tablets can be made with sugar, gelatin, hydroxypropylcellulose, nor acrylic resins. Tablets with a sustained action may laso be obtained using an excipient which provides regressive osmosis, such as the galacturonic acid polymers. Formulations for oral use may also be presented as hard capsules of absorbable material, such as gelatin, wherein the active ingredient is mixed with an inert solid diluent and lubricating agents, or pasty materials, such as ethoxylated saturated glycerides. Soft gelatin capsules are also possible wherein the active ingredient is mixed with water or an oily medium, for example peanut oil, liquid paraffin or olive oil.
Dispersible powders and granules suitable for the preparation of a suspension by the addition of water provide the active ingredient in admixture with a dispersing or wetting agent; a suspending agent, such as sodium carboxymethylcellulose, methylcellulose, hydroxypropylmethylcellulose, sodium alginate, polyvinylpirrolidone, gum tragacanath, xantham gum, gum acacia, and one or more preservatives, such as methyl or n-propyl p-hydroxybenzoate. Additional excipients, for example sweetening, flavouring and coloring agents may also be present.

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Liquid compositions for oral administration include emulsions, solutions, suspensions, syrups and elixirs containing commonly used inert diluents, such as distilled water, ethanol, sorbitol, glycerol, or propylene glycol. Aqueous solutions can also be prepared using P-cyclodextrin. Such compositions may also comprise adjuvants such as wetting agents, suspending agents, sweetening, flavouring, perfuming, preserving agents and buffers.
Other compositions for oral administration include spray compositions, which may be prepared by known methods. The spray compositions will contain a suitable propellent.
Preparations for injection, according to the present invention, for parenteral administration include sterile aqueous or non-toxic parentally-acceptable diluent or solvent. Examples of aqueous solvents or suspending media are distilled water for injection, Ringer's solution, and isotonic sodium chloride solution. Aqueous solutions can also be prepared using P-cyclodextrins, such as hydroxypropyl- β-cyclodextrin. Such compositions may also comprise adjuvants such as wetting agents, suspending agents, sweetening, flavoring, perfuming, preserving agents and buffers.
Other compositions for oral administration include spray compositions, which may be prepared by known methods. The spray compositions will contain a suitable propellent.
Preparations for injection, according to the present invention, for parenteral administration include sterile aqueous or non-aqueous solutions, suspensions or emulsions, in a non-toxic parentally-acceptable diluent or solvent. Examples of aqueous solvents or suspending media are distilled water for injection, Ringer's solution, and isotonic sodium chloride solution. Aqueous solutions can also be prepared using β-cyclodextrin, such as hydroxypropyl- β-cyclodextrin. Examples of non-aqueous solvents or suspending media are propylene glycol, polyethylene glycol, vegetable oils such as olive oil, or alcohols such as ethanol. These compositions may also include adjuvants such as wetting, preserving, emulsifying and dispersing agents. They may be sterilized by one of the known methods or manufactured in the form of sterile solid compositions which can be dissolved in sterile water or some other sterile injectable medium immediately before use. When all of the components are sterile, the injectables will maintain the sterility if they are manufactured in sterile environment.

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Preparations for vaginal administration according to the present invention include tablets, capsules, softgels, moulded pessaries, creams, foams and vaginal douches. Vaginal tablets provide the active component in admisture with microcrystalline cellulose, pregelatinized starch, lactose, microcrystalline cellulose, pregelatinized starch, polyvidone and magnesium stearate as typical excipients. Soft gelatin capsules (softgels) can be made dispersing the active ingredient in an oily medium, for example liquid paraffin, dimethylpolysiloxane 1000 or hydrogenated soybean oil. Moulded pessaries provide the active ingredient in admixture with a suitable synthetic or semisynehetic base (such as Suppocire® or Novata® types). Low viscosity saturated Cg to C12 fatty acid glycerides and colloidal silice are also added to improve incorporation and to prevent sedimentation of the active ingredient. Vaginal creams can be prepared as emulsions, with sufficient viscosity to retain their integrity and adhere to the vaginal cavity. Neutral fats, fatty acids, waxes, mineral oils and fatty acid esters can be used as the oily phase. Water, glycerine, sorbitol solution and polyethylene glycol are suitable excipients for the aqueous phase. Non-ionic emulsifying agents like polyethylene glycol ethers may also be used, and such compositions may also contain preserving, buffering and stiffening agents. Foaming systems can be made using a foamer (dispenser) that is able to transform a solution into a foam. Such systems may include cosolvents, buffers, preservatives, foam stabilizers and perfumes in an aqueous vehicle. Vaginal douches may contain cosolvents, preservatives, buffers and perfuming agents in a surfactant rich aqueous solution.
A compound of the invention may also administered in the form of suppositories for rectal administration of the drug, or as creams, ointments, pastes, lotions, gels, sprays, foams, aerosols, solutions, suspensions or powders for topical use. Such compositions are prepared following conventional procedures well known to those skilled in the art.
A compound of the invention may also be administered as a hair or body shampoo. These formulations may be prepared using suitable ionic and/or amphoteric surface-active agents such as sodium laureth sulfate, triethanolamine laureth sulfate, cocoamidopropyl betaine; thickening agents for example cocamide DEA, carbomer, sodium chloride and polyethylene glycol 6000 distearate; and optionally, emollient and superflatting agents, buffers, and preserving and perfuming agents.

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The dosage and frequency of dose may vary depending upon the nature and severity of the fungal disease, symptoms, age and body weight of the patient, as well as upon the route of administration. In general, the compounds of the invention will be administered orally or parenterally which can be administered as a single dose or as divided doses.
The invention is illustrated with the following examples and should not be construed to limit the scope of the present invention. The features of the present invention will become more apparent from the following description of the inventive concept and the description of the preferred embodiments and appended claims
EXAMPLES
General procedure: Preparation of compounds of formula (1) ,wherein R=H:
Example 1: Preparation of 6 and/or 7 substituted or unsubstituted-3-[2-( dihalophenyl)-2-hydroxy-3-(l,2,4)triazol-l-ylpropyl]-3H-thieno[3,2-d]pyrimidin-4-ones of formula(l):
A mixture of potassium carbonate or potassium hydroxide or sodium hydroxide (1.79 mmol), 6and/or7substituted or unsubstituted- thieno-[3,2-d]pyrimidin-4(3H)-one (0.89 mmol)(3), l[[2-(2,4-dihalophenyl)oxiranyl]methyl]-lH-l,2,4-triazole (1.79 mmol)(2) in ethyl acetate or methanol or t-butanol (20 ml) was refluxed for 12-22 hours. The reaction mixture was then cooled, organic solvent removed, reaction mixture diluted with water (25 ml) and extracted with organic solvent like chloroform, dichloromethane or ethyl acetate (2 x 20 ml). The combined organic layer was washed with brine and concentrated to yield the title compound 1)
Example II: Preparation of 6-Iodo - 3-[2-( difluorophenyl)-2-hydroxy-3-( 1,2,4)triazol-1 -ylpropyl]-3i/-thieno[3,2-d]pyrimidin-4-one [1A]
To the flame dried potassium carbonate (250 mg, 1.79 mmol) taken in two-neck RB flask under nitrogen atmosphere were added tetrabutylammonium bromide (350 mg, 1.08 mmol), 6-iodo- thieno-[3,2-d]pyrimidin-4(3H)-one (250 mg, 0.89 mmol), l[[2-(2,4-difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole (430 mg, 1.79 mmol) and dry ethyl acetate (20 ml). The reaction mixture was refluxed for 22 hours. The reaction mixture was

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then cooled, diluted with water (25 ml) and the two layers were separated. The aqueous, layer was extracted with ethyl acetate (20 ml), the combined organic layer was washed with brine and concentrated to get the desired product (150 mg, 33.18%). Yield: 33%; MP: 187°C; IR (Chloroform): v 3443, 3020,2400,1715 c-1; !H NMR (200 MHz, CDC13 + DMSO-δ 4.36(d, J=14 Hz, IH), 4.54 (d, J=14 Hz, IH), 4.65 (d, J=14 Hz, IH), 4.86(d, J = 14 Hz, IH), 6.27(bs, IH), 6.65-6.80(m, IH), 6.85-7.00 (m, IH), 7.20-7.35(m, IH), 7.49 (s, IH), 7.64(s, IH), 8.15(s, IH), 8.23 (s, IH); 13C NMR (50 MHz, CDCl3 + DMSO-de): 6 49.11, 53.25, 73.09, 102.44,109.12,121.52, 126.09,128.26, 132.74, 137.89,143.03,148.60, 154.26,155.00, 156.06,161.90,163.31. Spectral data:
Example III: 6-Bromo- 3-[2-( difluorophenyl)-2-hydroxy-3-(l,2,4)triazol-l-ylpropyl]-3//-thieno[3,2-d]pyrimidin-4-ones [IB]
6-bromo-thieno-[3,2-d]pyrimidin-4(3//)-one (3B) and l[[2-(2,4- difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole used as starting material and adapting the process described in example 1 to obtain the title compound. Yield: 40%; IR (CHCl 3): v 3351, 3020, 2400, 1666 cm-1; !H NMR (200 MHz, CDC13): 8 4.25 (d, J=14 Hz, IH), 4.54 (d, J=14 Hz, IH), 4.74(d, J=14 Hz, IH), 4.88(d, J=14 Hz, IH), 5.99 (bs, IH), 6.70-6.90 (m, 2H), 7.32 (s, IH), 7.50-7.58 (m, IH), 7.89 (bs, IH), 8.07 (s, IH), 8.24 (bs, IH);MS (ESI): (m/z) 468 and 470 (M+l), 490 and 492 (M+Na).
ExampleIV:)6-Iodo-7-bromo-3-[2-(difluorophenyl)-2-hydroxy-3-(l,2,4)triazol-l-ylpropyl]-3H-thieno[3,2-d]pyrimidin-4-ones [1C]
6-Iodo-7-bromo-thieno-[3,2-d]pyrimidin-4(3H)-one (3C) and l[[2-(2,4- difluorophenyl)oxiranyl]methyl]-lH-l,2,4-triazole used as starting material and adapting the process described in example 1 to obtain the title compound.
Yield: 75%; MP: 163°C; IR (Chloroform): v 3412, 3019,2400, 1676 cm-1; !H NMR (200 MHz, CDCI3): 5 4.06-4.98 (m, 4H), 5.95 (bs, IH), 6.70-7.15 (m, 2H), 7.45-7.75 (m, IH), 7.84 (bs, IH), 8.07 (bs, IH), 8.19 (bs, IH);
General procedure : Preparation of compounds of formula (1), wherein R=CH3:

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ExampleV: Preparation of 6,and/or7-substitutedor unsubstituted-3-[2-( difluoro-phenyl)-2-hydroxy-1 -methyl-3-( 1,2,4)triazol-1 -ylpropyl]-3//-thieno[3,2-d]pyrimidin-4-ones step 1:
A mixture of 6and/or7-substituted or unsubstituted thieno-[3,2-d]pyrimidin-4(3//)-one (1 mmol)(3), a suitable base like potassium carbonate (2 mmol), phase transfer catalyst like tetrabutylammonium bromide or tetrabutylammonium hydroxide or cetrimide (1.2 mmol) and organic solvent like ethyl acetate, dichloromethane (10 ml) was refluxed for 30 min., the solution of 2-bromo-l-(2,4-difluorophenyl)-l-propanone (1 mmol)(5) in organic solvent (1 ml) was added and refluxing was continued for 10-25 hours. The reaction mixture was then cooled, diluted with water (5 ml) and the two layers were separated. The aq. layer was extracted with ethyl acetate (2x5 ml), the combined organic layer was washed with brine and concentrated to obtain desired product.(6) step 2:
A mixture of KOH (2.2 mmol), water (0.2 ml), cetrimide (0.05 mmol), trimethyl sulfoxonium iodide (1.8 mmol) and DCM (4 ml) was stirred at 10-45°C for 30 min. A solution of 6and/or7-substituted or unsubstituted-3-{[2-(2,4-difluoro-phenyl)-2 oxo]-ethyl}-3H-thieno[3,2-d] pyrimidin-4-one compound (1 mmol) in DCM (2 ml) was added and the refluxing was continued for 10-25 hours. The reaction mixture was then cooled, diluted with water, the two layers were separated and the aqueous layer was extracted with DCM (20 ml). The combined organic extracts were washed with brine and concentrated to obtain product(7) step 3:
A mixture of sodium methoxide or sodium hydride or potassium carbonate (2.92 mmol), 1,2,4 triazole (0.20 g, 2.92 mmol) and product(7)(2.43 mmol) in dry t-BuOH, or methanol or ethyl acetate or DMF (50 ml) was stirred at 0-60°C for 12-20 h. Organic solvent (-45 ml) was removed on rotavapour, the residue was diluted with water (30 ml), extracted with ethyl acetate (2 x 50 ml), concentrated and purified by column chromatography to obtain product (1).
Example VI :6-Bromo-3-[2-(2,4-difluoro-phenyl)-l-methyl-2-oxo-ethyl]-3H-thieno[3,2-d]pyrimidin-4-one[6B]

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To the flame dried potassium carbonate (1.61 g, 11.68 mmol) taken in two-neck RB flask under nitrogen atmosphere were added tetrabutylammonium bromide (2.26 g, 7.01 mmol), 6-bromo- thieno-[3,2-d]pyrimidin-4(3H)-one (1.35 g, 5.84 mmol) and 50 ml dry ethyl acetate. The reaction mixture was refluxed for 30 min., the solution of 2-bromo-l-(2,4-difluorophenyl)-l-propanone (1.45 g, 5.84 mmol) in ethyl acetate (5 ml) was added and refluxing was continued for 25 hours. The reaction mixture was then cooled, diluted with water (25 ml) and the two layers were separated. The aq. layer was extracted with ethyl acetate (20 ml), the combined organic layer was washed with brine and concentrated to obtain the desired product (1.6g, 68.9%) as a yellow solid.
Yield: 68.9%; *H NMR (200 MHz, CDC13): 51.75 (d, J= 6Hz, 3H), 6.06 (q, J=6 Hz, IH), 6.81-7.02 (m, 2H), 7.30 (s, IH), 7.89-7.98 (m, IH), 8.11 (s, IH)
Example VII:6-Bromo-3-{l-[2-(2,4-difluoro-phenyl)-oxiranyl]-ethyl}-3H-thieno[3,2-d]pyrimidin-4-one[7B]
KOH (0.33 g, 6.06 mmol) in water (0.5 ml) was taken in 100 ml RB flask, cetrimide (0.05 g, 0.13 mmol), trimethyl sulfoxonium iodide (1.09 g, 4.96 mmol) and DCM (10 ml) were added and the reaction mixture was stirred at 45 °C for 30 min. A solution of 6-bromo-3-{l-[2-(2,4-difluoro-phenyl)-2 oxo]-ethyl}-3H-thieno[3,2-d] pyrimidin-4-one compound (1.10 g, 2.75 mmol) obtained in example VI in DCM (5 ml) was added and the refluxing was continued for 25 hours. The reaction mixture was then cooled, diluted with water, the two layers were separated and the aqueous layer was extracted with DCM (20 ml). The combined organic extracts were washed with brine and concentrated to obtain oxiranyl compound (0.802 g, 70.37%) as a yellow solid.
IR (Chloroform): v 3020, 2400, and 1681 cm-1; 1H NMR (200 MHz, CDC13): 81.50 (d, J= 8 Hz, 3H), 2.61 (d, J=4 Hz, IH), 2.73 (d, J=4 Hz, IH), 5.89 (q, J=8 Hz, IH), 6.81-6.97 (m, 2H), 7.33 (s, IH), 7.36-7.52 (m, IH), 8.07 (s, IH); 13C NMR (50 MHz, CDCI3): 6 15.90, 48.62, 51.77, 58.78, 104.30, 111.67, 120.62, 124.19, 124.69, 127.99,129.84, 131.60, 146.15, 155.60, 156.17, 165.71.
ExampleVIII:6-Bromo-3-[2-(difluorophenyl)-2-hydroxy-l-methyl-3-(l,2,4)triazol-l-ylpropyl]-3//-thieno[3,2-d]pyrimidin-4-ones:[lF]

27
Products of examples VI and VII were contacted under the condition of step3 of example
V to obtain the title compound.
Yield: 44 %; !H NMR (200 MHz, CDC13): δ1.29 (d, J=6 Hz, 3H), 3.96 (d, J=10 Hz, 1H),
5.16(d, J=10 Hz, 1H), 5.92 (q, J=6 Hz, 1H), 6.70-6.90 (m, 2H), 7.27, 7.38 (s, 1H), 7.42-
7.52 (m, 1H), 7.74 (s, 1H), 7.83 (s, 1H), 8.56, 8.74 (s, 1H).
Example IX: 6,7-dibromo-3-[2-(2,4-difluoro-phenyl)-l-methyl-2-oxo-ethyl]-3j^-
thieno[3,2-d]pyrimidin-4-one[6C]
To the flame dried potassium carbonate (1.07 g, 7.8 mmol) taken in two-neck RB flask
under nitrogen atmosphere were added tetrabutylammonium bromide (1.51 g, 4.6 mmol),
6,7-dibromo- thieno-[3,2-d]pyrimidin-4(3H)-one (1.21 g, 3.9 mmol) and 50 ml dry ethyl
acetate. The reaction mixture was refluxed for 30 min., the solution of 2-bromo-l-(2,4-
difluorophenyl)-l-propanone (0.97 g, 3.9 mmol) in ethyl acetate (5 ml) was added and
refluxing was continued for 22 hours. The reaction mixture was then cooled, diluted with
water (25 ml) and the two layers were separated. The aq. layer was extracted with ethyl
acetate (20 ml), the combined organic layer was washed with brine and concentrated to get
the desired product (1.1 g, 58.4 %) as a yellow solid.
Yield: 58.4 %; *H NMR (200 MHz, CDCI3): 61.79 (d, J= 8 Hz, 3H), 6.13 (q, J=8 Hz, 1H),
6.75-7.20 (m, 2H), 7.80-8.20 (m, 1H), 8.25 (s, 1H).
Example X: 6,7-Dibromo-3-{l-[2-(2,4-difluoro-phenyl)-oxiranyl]-ethyl}-3/7-thieno[3,2-d]pyrimidin-4-one[7C]
KOH (0.29 g, 5.2 mmol) in water (0.5 ml) was taken in 100 ml RB flask, cetrimide (0.08 g, 0.2 mmol), trimethyl sulfoxonium iodide (1.06 g, 4.8 mmol) and DCM (10 ml) were added and the reaction mixture was stirred at 45°C for 30 min. A solution of 6,7-dibromo-3-{l-[2-(2,4-difluoro-phenyl)-2 oxo]-ethyl}-3H-thieno[3,2-d] pyrimidin-4-one compound (1.15 g, 2.4 mmol) in DCM (5 ml) was added and the refluxing was continued for 21 hours. The reaction mixture was then cooled, diluted with water, the two layers were separated and the aqueous layer was extracted with DCM (20 ml). The combined organic extracts were washed with brine and concentrated to get the product (0.81 g, 69.2%) as a yellow solid.

28
IR (Chloroform): v 3019, 2400, and 1679 cm-1; 1H NMR (200 MHz, CDC13): 61.51 (d, J= 8 Hz, 3H), 2.60 (d, J=4 Hz, IH), 2.73 (d, J=4 Hz, IH), 5.89 (q, J=8 Hz, IH), 6.70-7.00 (m, 2H), 7.30-7.50 (m, IH), 8.19 (s, IH).
Example XI: Preparation of 6,7-Dibromo-3-[2-(difluorophenyl)-2-hydroxy-l-methyl-3-(1,2,4)triazol-1 -ylpropyl]-3H-thieno[3,2-d]pyrimidin-4-ones: [1G] A mixture of sodium methoxide (0.15 g, 2.92 mmol), 1,2,4 triazole (0.20 g, 2.92 mmol) and dibromoepoxide (1.00 g, 2.43 mmol) in dry t-BuOH (50 ml) was heated under reflux for 12 h. t-BuOH (-45 ml) was removed on rotavapour, the residue was diluted with water (30 ml), extracted by using ethyl acetate (2 x 50 ml) and concentrated to get the pale yellow coloured solid product (0.51 g, 44%).
IR (Nujol): v 3358, 2400, 1672 cm-1; 1H NMR (200 MHz, CDCI3): 51.30 (d, J= 6Hz, 3H), 3.95 (d, J=14 Hz, IH), 5.13 (d, J=14 Hz, IH), 5.60 (s, IH), 5.93 (q, J= 6 Hz, IH), 6.70-6.92 (m, 2H), 7.41-7.56 (m, IH), 7.74 (s, IH), 7.78 (s, IH), 8.70(s, IH); 13C NMR (50 MHz, CDCl3 + DMSO-d6): 6 13.65,49.87,52.76,75.07, 102.17, 108.95, 109.00, 111.50, 120.55, 121.80, 127.78, 147.35, 151.02, 153.95, 157.72, 162.58, 168.26,190.74.
Yield: 21%; IR (Chloroform): v 3387, 3019,2400, 1674cm-1; 1H NMR (200 MHz, CDCI3): 6 1.31(d J=6 Hz, 3H), 3.96(d, J=14 Hz, IH), 5.16(d, J=14 Hz, IH), 5.58(s, IH); 55.97q, J=6 Hz, IH), 6.72-6.93 (m, 2H), 7.40-7.60 (m, IH), 7.75 (s, IH), 7.78 (s, IH), 7.85 (s, IH); 8.75 (s, IH); 13C NMR (50 MHz, CDC13): 5 15.58, 51.24, 54.12, 77.98, 104.44, 111.92, 122.16,122.65, 130.32, 131.83, 144.04, 148.11, 151.96, 153.31, 157.31, 160.38, 165.37, 165.69. MS (ESI) (m/z): 482 and 484 (M+).
The following compounds were prepared by the same method.
ExampleXII:Preparation of 3-[2-( difluorophenyl)-2-hydroxy-l-methyl-3-(l,2,4)triazol-l-ylpropyl]-3H-thieno[3,2-d]pyrimidin-4-ones:[lE]

29
2-bromo-l-(2,4-difluorophenyl)-l-propanone and compound 3E are used as starting materials. Following the steps 1,2 and 3 of example V yielded the title compound . Yield: 46%; MP: 160°C; *H NMR (200 MHz, DMSO-de): 51.49 (d, J= 4 Hz, 3H), 4.42 (d, J=10 Hz, IH), 5.15 (d, J=10 Hz, IH), 6.18 (q, J= 4 Hz, IH), 6.66 (s, IH), 7.20-7.30 (m, IH), 7.45-7.65 (m, 2H), 7.75 (d, J=4 Hz, IH), 7.86 (s, IH), 8.40-8.60(m, 2H), 8.74 (s, IH); 13C NMR(75 MHz, DMSO-de): 5 15.48, 51.04, 54.49, 77.25, 104.02, 110.82, 111.10, 121.96, 124.95,129.59,135.82,147.30,150.32,156.27(2C), 157.24(2C), 163.78. MS(m/z):404(M+l).
Example XIII:Preparation of 6-Iodo-3-[2-( difluorophenyl)-2-hydroxy-l-methyl-3-(1,2,4)triazol-1 -ylpropyl]-3i/-thieno[3,2-d]pyrimidin-4-ones [1J]: 2-bromo-l-(2,4-difluorophenyl)-l-propanone and compound 3A are used as starting materials. Following the steps 1,2 and 3 of example V yielded the title compound Yield: 20%; MP: >200 °C; IR (CHC13): v 3400, 3019, 2400, 1673 cm-1; 1H NMR (200 MHz, CDCI3): 5 1.30 (d, J=6 Hz, 3H), 3.96 (d, J=14 Hz, IH), 5.15 (d, J=14 Hz, IH), 5.57 (s, IH), 5.92 (q, J=6 Hz, IH), 6.75-6.90 (m, 2H), 7.40-7.55 (m, IH), 7.57 (s, IH), 7.73 (s, IH), 7.77 (s, IH), 8.51 (s, 1H);MS (m/z): 530 (M+l), 552 (M+Na).
Example XIV: Prepatration of 6-Iodo-7-Bromo-3-[2-( difluorophenyl)-2-hydroxy-l-methyl-3-(l,2,4)triazol-l-ylpropyl]-3//-thieno[3,2-d]pyrimidin-4-ones[ 1K] 2-bromo-l-(2,4-difluorophenyl)-l-propanone and compound 3C are used as starting materials. Following the steps 1,2 and 3 of example V yielded the title compound. Yield: 19%; MP: 178 °C; IR (CHC13): v 3394, 2253, 1674 cm-1; 1H NMR (200 MHz, CDCI3): δ 1.28, 1.32 (d, J=8 Hz, 3H), 3.97 (d, J=14 Hz, IH), 5.13 (d, J=14 Hz, IH), 5.63 (bs, IH), 5.92 (q, J=8 Hz, IH), 6.70-6.95 (m, 2H), 7.47-7.60 (m, IH), 7.74 (s, IH), 7.84 (s, IH), 8.63, 8.66 (s, IH).
ExampleXV: Preparation of 6-(l,2,4-Triazolyl)-7-Bromo-3-[2-(difluorophenyl)-2-hydroxy-1 -methyl-3 -(1,2,4)triazol-1 -ylpropyl] -3i/-thieno[3,2-d]pyrimidin-4-ones: [ 1L] 1,2,4- Triazole (173 mg, 2.50 mmol) was added portionwise under nitrogen atmosphere to a mixture of NaH (52 mg, 2.15 mmol) in DMF (5 ml) at 0°C. The mixture was stirred at RT for 30 min. and the solution of 6,7-dibromo oxiranyl (7C,425 mg, 0.86 mmol in DMF (2 ml) was added. The reaction mixture was stirred at 85°C for 25 h, cooled and poured in 25 ml of water. It was then extracted with ethyl acetate (2 x 20 ml), washed with water and concentrated to give the crude product. Purification by column chromatography afforded the pure product.

30
Yield: 32%; IR (Nujol): v 3355, 2900, 1669cm-1; 1H NMR (200 MHz, CDC13): δ1.32(d, J=6 Hz, 3H), 4.00(d, J=14 Hz, 1H), 5.15(d, J=14 Hz, 1H), 5.65(s, 1H), 5.96(q, J=6 Hz, 1H), 6.76-6.90(m, 2H), 7.45-7.52(m, 1H), 7.75(s, 1H), 7.80(s, 1H), 8.17(s, 1H), 8.77(s, 1H), 9.28(s, 1H);MS (m/z) 549 and 551(M+1), 571 and 573 (M+Na).
Antifungal Activity Testing:
The compound of Formula (I) and their pharmaceutically acceptable salts are antifungal agents effective to a greater or lesser extent, and useful in treating fungal infectionsin animals and humans, especially those caused by Calibicans, Aspergillus andFusarium.
In vitro evaluation of antifungal activity can be performed by determining the minimum inhibitory concentration.
Anti-fungal susceptibility testing of these anti-fungal compounds was done by conventional method using soyabean casein digest broth. Known anti-fungal agents like Fluconazole and amphotericin-B were used as positive control. End points were determined after 48 hours visually and by using Spectrophotometer wherever necessary. Different dilutions were tried and the set of experiments.
Antifungal activity of these compounds also extends to Aspergillus and Fusarium. The activity seen in compound of Formula 1) as against these strains suggests that it exhibits broad spectrum antifungal activity.
The results are enumerated in the table below:

31

Sr Code no Structure Activity against organisms
no In ug/ml
C. albicans A. niger F. proliferatum
01 ID R = R1=R2 = H 0.5 128 NA
02 IE R = Me,Rl=R2 = H 0.25 8 NA
03 IF R = Me,Rl=Br, R2 = H 0.12 4 NA
04 1J R = Me, Rl -1, R2 = H 0.03 1-2 NItill 16
05 IK R = Me, Rl = I, R2 = Br 0.12-0.25 NItilU NItill 4
06 1H R = Me, Rl = H, R2 = Br 0.06-0.12 NI till 8 NItill 8
07 R = Me,Rl = 0.12- NItill NItill 16
IL l(l,2,4-triazolyl), R2 = Br 0.25 16
08 IG R = Me,Rl=R2 = Br 0.06-0.12 NItill 2 NItill 2
19 IB R = R2 = H,R1 = Br 0.06 32 NA
10 1A R = R2=H, Rl = I 0.06 32 NA
11 IC R = H, Rl =1, R2 = Br 1 NA NA
Main Advantages of the Invention:
1.Compounds of present invention exhibit broad spectrum anitifungal activity.
2. Better activity against Candida strains resistant to known azoles.
3. Compounds possess activity against aspergillus and other emerging fungal
pathogens.
4. Better safety profile than earlier azoles at the same time retaining its broad spectrum of activity.

32
We claim
1) Compounds represented by formula (I)

R1
w

F\=/ R2




R1
FW/ R2
, base

Formula (1)
Wherein R = Me and the remaining radicals Ri and R2 each independently of others hydrogen or halogen or carboxyl or alkyl carboxyl or carboxyester or alkyl carboxyester or alhyl cyono or 1-(1, 2,4 triazolyll), its solvates or its salts of such compounds having at least one salt forming group.
Wherein R = H, and the remaining radicals R1 and R2 each independently of others hydrogen or halogen or carboxyl or alkyl carboxyl or carboxyester or alkyl carboxyester or alkyl cyano or 1 -(1,2,4 triazolyl) or represent CI -C4 alkyl, C.3 -C.6 cycloalkyl, CI -C4 haloalkyl, CI -C.4 alkoxy, CI -C4 haloalkoxy, halogen, nitro, cyano, hydroxy, benzyloxy, hydroxymethyl, NR, -CONR, CH.2 -OCO-R., CO--R4, --SO.,-CNHR, 1-pyrrolyl, 1-imidazolyl, lH-l,2,4-triazol-l-yl, 5-tetrazolyl, 1-pyrrolidinyl, 4-morpholinyl, 4-morpholinyl-N-oxide.

33
2) A compound of formula (I) according to claim 1, wherein
R = H , R1=R.2= H,Br and/or I, its solvates and pharmaceutically acceptable salt such compounds having at least one salt forming group.
R= Me,R1 = R2 = H, Br, I and / or 1 - (1,2,4 - Triazolyl), its solvates and pharmaceutically acceptable salt of such compounds having at least one salt forming group. 3 .A pharmaceutical composition comprising a compound of formula (I) according to any of claims 1 and 2 or its solvates or pharmaceutically acceptable salts of such compound having at least one salt forming group together with a pharmaceutical carrier.
4) A pharmaceutical composition in capsule or form to compound of claim 1 or its solvates or its pharmaceutically acceptable salt of said compound having at least one salt forming group thereof with pharmaceutically acceptable diluents or carrier thereof
5) A method for the treatment or prevention of a fungal infection in a substrate,said method comprising administering a compound of formula 1 as claimed in claim l or a pharmaceutically acceptable salt of such compound having at least one salt forming group or solvate thereof to a substrate in need of such treatment or prevention.
6) The method of claim 5, wherein the said substrate is animal or human being.

7) A pharmaceutical composition according to claim 3 for the treatment or prevention of fungal infections
8) A process for the preparation of compound of formula (I), wherein R=H to claim 1 or its solvate or pharmaceutically acceptable salt of such compound having at aleast one salt forming group, said process comprising steps of:
a) contacting oxiranyl compound of formula (2),

34

Formula (2)
with thienopyrimibone compound of formula(3) in an organic solvent in presence of base and a catalyst
\==/"rc
Formula (3)
Wherein R1 and R2 each independently of others defined for R being H as above .
b)to obtain compound of formula (1), and

R Q

S^ ^R1

Formula (1)
R1 and R2 each independently of others defined for R being H as above
c) converting the compound of formula (1) to its pharmaceutically acceptable salt by adapting conventional method..

35

9) A process of claim 8, wherein in step(a) the organic solvent used is selected from
the group consisting of esters, alcohols and chlorinated hydrocarbons preferably ethyl
acetate- or dichloromethane- or t- butanol.
10) A process of claim 8, wherein in step (a) the base used is selected from the group consisting of alkali hydroxides and carbonates, preferably potassium carbonate or potassium hydroxide.
11) A process of claim 8,wherein in step(a) the phase transfer catalyst used is selected from the group consisting of tetraalkyl ammonium compounds , preferably cetrimide.
12) A process for the preparation of compound of formula (I), wherein R=Me to claim 1 or its solvate or pharmaceutically acceptable salt of such compound having atleast one salt forming group, said process comprising steps of:
a) contacting compound of formula (5)
R O,
Formula (5)
with thienopyrimidone compound of formula(3) in an organic solvent in presence of base and a catalyst,
\=/ R2
Formula (3)
Wherein R1 and R2 each independently of others defined for R being Me as above
b) to obtain compound of formula (6),

36

Formula (6)
Wherein R1 and R.2 each independently of others defined for R being Me as above
c) contacting compound (6) of step (b) with trimethylsulfoxinium iodide in an organic solvent containing aqueous base, phase transfer catalyst at a temperature ranging between 10° C to 45°C to obtain compound of formula(7),

Formula (7)
Wherein R1 and R2 each independently of others defined for R being Me as above
d) contacting compound (7) with 1,2,4-triazole in an organic solvent in presence of a base at a temperature ranging between 0° to 60° C for a time period of 10 to 25 h to yield compound of formula (1), and

37

Formula (1)
wherein R1 and R2 each independently of others defined for R being Me as above
e)converting the compound of formula (1) to its pharmaceutically acceptable salt by adapting conventional method..
13) A process of claim 12, wherein the organic solvent used is selected from the group consisting of-esters ;alcohols andchlorinated hydrocarbons,preferably- ethyl acetate, dichloromethane- and t- butanolokay
14) A process of claim 12, wherein the base used is selected from the group
consisting of alkalihydroxides and alkali carbonates,preferably
potassium hydroxide and potassium carbonate
15) A process of claim 12, wherein the phase transfer catalyst used is selected
from the group consisting of tetraalkyl ammonium compounds ,
preferably cetrimide
16) An intermediate compounds of formula 6A,6B,6C,6D and 6E.
17) An intermediate compounds of formula 7A,7B,7C,7D and 7E.
18) A use of a compound of formula (I) according to any of claims 1 to 2 or its
solvates or a pharmaceutically acceptable solt of said compound having at least
one salt forming group for the preparation of a pharmaceutically composition for
use in the treatment of antifungal infections.

38
19) Compound of formula (1) of claim 1 as herein described substantially with reference to chemical formula.
20) Process for the preparation of compound of formula (1) as herein substantially described with reference to examples