The present invention discloses a novel a process for the preparation of (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2-(I-tetrahydropyrimid-2-onyl)-3-methylbutanoyl)-amino-l,6-diphenylhexane of formula I comprising condensing N-[(lS,2S,4S)-4-amino-2-hydroxy-5-phenyl-l-(phenylmethyl)pentyl]-2-(2,6-dim...
The present invention relates to a novel, cost-effective process for the preparation of an anti-parasitic drug febantel of formula I involving a novel intermediate.
The present invention relates to a new method for preparing 4,4"-(l-methyl-1,2-ethandiyl)-bis-(2,6-piperazinedione) of formula (I) or its enantiomers. More specifically this invention relates to a new process for preparing 4,4"-( 1-methyl-1,2-ethandiyl)-bis-(2,6-piperazinedione), which gives better yield and purity ...
The present invention discloses a novel, cost-effective process for the preparation of an Oxyclozanide. Specifically, it relates to the process for the preparation of anthelmintic drug. The process comprises a) conversion of 3,5,6- trichlorosalicylic acid to 3,5,6-trichloro-2-hydroxybenzoyl chloride with thionyl chl...
The present invention relates to a novel process for preparing an antiretroviral drugl,3-thiazol-5-yImethyl N-[(2S,3S,5S)-3-hydroxy-5-[(2S)-3-methyl-2- {[methyl({ [2-(propan-2-yl)-1,3-thiazol-4-yl]methyl })carbamoyI] amino}butanamido]-l,6-diphenylhexan-2-yl]carbamatecommonly known as Ritonavir of formula I, which co...
The present invention discloses a novel, cost-effective process for preparing psychostimulant drug cytidinediphosphate-choline (CDP-Choline) commonly known as citicoline. The process comprises reacting cytidine 5"-monophosphate with morpholine in presence of a coupling reagent and an organic solvent to form morpholi...
The present invention discloses a novel, cost-effective process for
preparation of a 2-cyclohexylcarbonyl-4-oxo-l,2,3,6,7,l 1b-hexahydro-4H-
pyrazino[2,l-a]isoquinoline formula I, which comprises: acylation of 4-oxo-
1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with
cyclohexanoylchloride in presence of...
The present invention relates to a novel process for the preparation of triaryl phosphite, specifically it relates to the process for the preparation of tris (2,4 -di-tert-butyl phenyl) phosphite of formula I, an antioxidant.
The present invention relates to a novel, cost-effective process for preparation of an anthelmintic drug. Specifically, it relates to a process for the preparation of l-(4-Isothiocyanatophenoxy)-4-nitrobenzene of formula I, commonly known as Nitroscanate.
The present invention relates to a novel process for the preparation of a non-steroidal anti-inflammatory drug, commonly known as carprofen of formula I.
The present invention discloses a novel, cost-effective one pot process for preparation of phenyl butyric acid of formula I by condensing phenyl ethyl bromide with diethyl malonate in presence of base and catalyst; insitu hydrolyzing the diethyl (2-phenyIethyl) malonate using a base to form diacid; and further decar...
The present invention relates to a novel, cost-effective process for preparation of an anthelmintic drug. Specifically, it relates to a process for the preparation of 4-amino-6-(trichloroethenyl)-l,3-benzenedisulfonamide of formula I, commonly known as Chlorsulon.
The present invention discloses a novel, cost-effective process for preparation of a diazoamino benzene compound. Specifically, it relates to the process for the preparation of diminazene diaceturate. The process comprises a) converting p-nitro benzoic acid of formula VII into p-nitro benzamide of formula VI; b...
The present invention discloses a novel, cost-effective process for preparation of a diazoamino benzene compound. Specifically, it relates to the process for the preparation of diminazene diaceturate. The process comprises a) converting p-nitro benzoic acid of formula VII into p-nitro benzamide of formula VI; b) con...
The present invention relates to a novel, cost-effective process for the preparation of Sterile Meropenem Trihydrate, which is prepared by a) condensation of l-Azabicyclo[3.2.0]hepta-2-ene-2-carboxylic acid, 3-[(diphenoxyphosphinyl)oxy]-6-(l-hydroxyethyl)-4-methyl-7-oxo-(4-nitrobenzyl) methyl ester,[4R-[4a,5b,6b(R*)...
The present invention relates to a novel process for the preparation of 1 β-methylcarbapenem antibiotic, Ertapenem of formula I. The process comprises deprotection of monoprotected Ertapenem acid or its monosodium salt by 2.5% Pd/C to obtain Ertapenem monosodium.
The present invention relates to a novel, cost-effective process for the preparation of a cholelitholytic agent Ursodeoxycholic acid of formula I, comprising reducing 7-ketolithocholic acid of formula II using a reducing agent and an alkoxide in presence of a solvent to obtain crude Ursodeoxycholic acid; and purifyi...
The present invention discloses a novel, cost-effective process for preparation of [R-[R*,R*-(E)]]-2,2'-(l,8-dioxo-4-octene-l,8-diyl) bis(oxy-3,1 -propanediyl) bis(l ,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1 -[(3,4,5-trimethoxyphenyl)- methyl] isoquinolinium) dichloride, commonly known as mivacurium chloride, which...
The present invention discloses a novel process for the preparation of (2S, 3S, 5S)-5-amino-2-(N-((5-thiazolyl)-methoxycarbonyl)amino)-l,6-diphenylhexane hydrochloride of formula II, which is a key intermediate in the preparation of cobicistat, a drug under experimental investigation for use in the treatment of infe...
The present invention provides an improved process for preparation of Firocoxib of Formula I. Further, the present invention relates to novel process for the preparation of crystalline polymorphic form B of Firocoxib of Formula I.
The present invention relates to a novel, cost-effective process for the preparation of 1-hydrazinophthalazine hydrochloride of formula I, which involves the preparation of 1-chlorophthalazine using phthalazinone and phosphorous oxychloride, further reacting with hydrazine hydrate and an acid followed purification o...
The present invention discloses a novel process for the preparation of ethyl 3-[5-(3-chloro-2-fluorobenzyl)-2.4-dimethoxy phenyl]-3-oxopropanoate of formula II, which is a key intermediate in the preparation of Eivitegravir, a drug used in the treatment of infection with the human immunodeficiency virus (HIV).
...
The present invention relates to a facile and cost-effective process for the preparation of ether derivatives of dihydroartemisinin. The present invention farther enables preparation of pure ß-ether derivatives of dihydroartemisinin, commonly known as Artemether, the methyl ether derivative and Arteether, the ethyl ...
The present invention relates to a novel process for the preparation of Succinylcholine Chloride, a pharmaceuticaliy active compound used as skeletal muscle relaxant which comprises condensing succinic anhydride with N,N-Diemthylaminoethanol using a catalyst in presence of a solvent to form bis[2-(dimethylamino)ethy...
The present invention relates to a novel, cost-effective process for preparation of an Antioxidant bis (2,4-dicumyIphenyI) pentaerythritol diphosphite commonly known as Doverphos-S-9228 of formula I by condensing pentaerythritol with 2,4-dicumylphenol using a reagent and catalyst in presence of a solvent.
...
The present invention discloses a novel, cost-effective process for preparation of 4-(propylthio)benzene-l,2-diamine of formula II, a key intermediate of an anti-parasite bulk drug albendazole.
The present invention relates to a novel process for preparation of 2-((4-tert-butylcyclohexyl)methyl)-3-hydroxy-1.4-naphthoquinone commonly known as Buparvaquone of formula I without using silver nitrate as a catalyst.
The present invention discloses a novel, cost-effective process for preparation of a benzimidazole carbamates compound. Specifically, it relates to the process for the preparation of anti-parasite bulk drug albendazole. The process comprises a) thiocyanating 2-nitroaniline of formula VI with ammonium thiocyanated in...
The present invention discloses a method for preparing Triclabendazole comprising
condensing N-(4,5-dichloro-2-nitrophenyl)acetamide with 2,3-dichlorophenol to
obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide and it to obtain 4-
chloro-5(2,3-dichlorophenoxy)-2-nitroaniline; reducing 4-chloro-5(2,3-d...
The present invention relates to a novel process for the preparation of an anaesthetic drug Midazolam of formula I which comprises reductive amination of l-{4-chloro-2-[2-(2-fluorophenyI)-l,3-dithioIan-2-yl]phenyl}-5-methyl-lH-imidazole-5-carboxaldehyde using a reducing agent and ammonia in an alcoholic solvent to o...
The present invention relates to a novel process for the preparation of cilastatin of formula I by the condensation of 7-chloro-2-[[(lS)-2,2-dimethylcyclopropane] carboxamide]-2-heptenoic acid with L-cysteine in presence of l,8-diazabicyclo[4.3.0]undec-7-ene (DBU) and a solvent.
The present invention relates to a novel cost effective and commercially viable process for the preparation of pure crystalline Imipenem monohydrate by dissolving crude imipenem in carbonated water and morpholinopropane sulphonic acid (MOPS); treating with carbon, filering and precipitating by an organic solvent.
...
The present invention disclosed a process for the preparation of etomidate in which the R-(+)-phenylethylamine is reacted with ethyl chloroacetate in absence of a solvent to give R-(+)-N-[(ethoxycarbonyl)methyl]-l-phenylethylamine, which is formylated to give R-(+)-(N-formyl-N-[(ethoxycarbonyl)methyl]-l-phenylethyla...
The present invention discloses a novel, cost-effective process for preparation of a 4- oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline derivatives. Specifically it discloses a process for the preparation of anthelmenthic drug praziquantel incorporating a novel intermediate 2-[(2,2-dimethoxyethyl)benzyl ...
Disclosed herin, an improved process for producing beta-thymidine from 5-methyl uridine.The process comprising cyclizing 5-methyl urdine to 2.2' anhydrothymidine, hydrohalogenating 2.2'-anhydrothmidine to from 2'halo-2'deoxy-5-methyl uridine resultant crude beta-thymidine to obtain pure beta-thymidine
...
Disclosed herein is an economical and enantioselective process for producing (S)-1-(2-amino-5-chlorophenyl)-1-(trifluoromethyl)-3-cyclopropyl-2-propane-1-ol comprising reacting 1-(2-amino-5-chlorophenyl)-2,2,2-trifluoroacetophenone, chiral zinc alkoxide and cyclopropyl acetylene followed by isolation and purificatio...
The present invention provides novel intermediates for producing pure doxercalciferol. Further, the process for producing said intermediates and use thereof in production of doxercalciferol is also disclosed herein.
The present invention discloses a stable amorphous form of Rifaximin characterised by having X-ray powder diffraction pattern as given in figure 1, having a 2θ peaks at 7.2 and having moisture content in the range of 3% to 4% preferably, 3.4% to 3.7%. This invention also discloses a novel process for its preparation...
The present invention relates to a novel in-situ process for preparing l-(6-methylpyridin-3-yl)-2-[(4-(methylsulphonyl)phenyl]ethanone of the formula I,which eliminates the isolation of ketosulfide stage and avoids use of methanesulfonic acid and alkali metal tungstate for the oxidation of ketosulfide to ketosulfone...
The present invention discloses a process for preparation of 1,3-Bis[3-(4,5-dihydro-lH-imidazol-2-yl)phenyl]urea dipropionate. The process comprises reacting 3-amino benzonitrile with carbonyl diimidazole in presence of an organic base and solvent to form l,3-Bis-(3-cyano-phenyl)-urea; cyclizing l,3-Bis-(3-cyano-phe...
The present invention discloses a novel, facile and cost-effective process for the preparation of (2E)-3-(4-amino-3,5-dimethylphenyl)acrylonitrile of formula II, which is a key intermediate in the preparation of an antiretroviral drug Rilpivirine.
The present invention discloses a novel process for the preparation of ethyl 3-{5-(3-chloro- 2-fluorobenzyl)-2,4-dimethoxy phenylj-3-oxopropanoate, which is a key intermediate in the preparation of Elvitegravir, a drug under experimental investigation for use in the treatment of infection with the human immunodefici...
The present invention discloses a novel, facile and cost-effective process for the preparation of an antihypertensive agent labetalol hydrochloride of formula I which comprises condensing l-methyl-3-phenyl propylamine with 5-bromo acetyl salicylamide in presence of solvent and hydrochloric acid to obtain 2-hydroxy-5...
The present invention relates to a novel in-situ process for preparation of . 2-((4-tert-butylcyclohexyl)methyl)-3-hydroxy-l,4-naphthoquinone commonly known as Buparvaquone of formula I. The buparvaquone is obtained in pure trans form by purification with a ketonic solvent.
The present invention relates to a novel process for preparing an antimalarial drug 2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-(4- chlorobenzylidene)-9H-fluoren-4-yl]ethanolcommonly known as Lumifantrine of formula I, which comprises:chloroacylating 2,7-dichloro-9H-fluorene using chloroaetyl chloride and a catalyst in ...
The present invention relates to a novel process for preparing (2E,4E,6E,8E)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoic acid of formula I, which avoids the isomerisation of cis-isomers.
The present invention relates to a novel crystalline form of 1-methylcarbapenem antibiotic, Ertapenem monosodium. The process comprises isolation of monoprotected Ertapenem acid or its monosodium salt and further deprotection to obtain Ertapenenm monosodium.
The present invention relates to a novel process for preparing 4-[3-[[2-Hydroxy-2-(4-hydroxyphenyl)ethyl] amino] butyl]phenol hydrochloride of formula I.
The present invention relates to a new amorphous form of tetrakis-(2,4-di-t-butylphenyl)-4,4"-biphenylene diphosphonite and a process of its preparation.
The present invention relates to a novel process for the preparation of triaryl phosphite, specifically it relates to the process for the preparation of tris (2,4 -di-tert-butyl phenyl) phosphite of formula I, an antioxidant.
The present invention relates to a novel process for the preparation of an anaesthetic drug Midazolam of formula I which comprises reductive amination of l-{4-chloro-2-[2-(2-fluorophenyl)-l,3-dithiolan-2-yl]phenyl}-5-methyl-lH-imidazole-5-carboxaldehyde using a reducing agent and ammonia in an alcoholic solvent to o...
The present invention discloses a novel, cost-effective process for preparation of sodium phenyl butyrate by treating a solution of a sodium salt of weak acid with phenyl butyric acid in an organic solvent in presence of a base under inert atmosphere.
The present invention relates to a novel, cost-effective and simple process for commercial scale production of methoxsalen which obviates the use of column chromatography for purification of dealkylated mass obtained from Ammi majus plant extract to obtain purified dealkylated mass enriched with methoxsalen and xant...
The present invention relates to a novel process for the preparation of 1-methylcarbapenem antibiotic, Ertapenem of formula I. The process comprises isolation of monoprotected Ertapenem acid or its monosodium salt and further deprotection to obtain Ertapenem monosodium.
The present invention relates to a facile and cost-effective process for the preparation of ether derivatives of dihydroartemisinin. The present invention further enables preparation of pure β-ether derivatives of dihydroartemisinin free from ά-isomer, commonly known as Artemether, the methyl ether derivative and Ar...
Abstract
The present invention discloses a novel, cost-effective process for the preparation of crystalline polymorphic Albendazole Form-I. The process comprises drying the wet albendazole having mixture of polymorphic forms under vacuum; heating and cooling to get pure crystalline Albendazole Form-1.
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The present invention discloses a novel, cost-effective process for preparation of [R-[R*,R*-(E)]]-2,2"-(1,8-dioxo-4-octene-1,8-diyl) bis(oxy- 3,1 -propanediyl) bis( 1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1 -[(3,4,5- trimethoxyphenyl)- methyl] isoquinolinium) dichloride, commonly known as mivacurium chloride. The...