FORM-2
THE PATENTS ACT, 1970 (39 of 1970)
&
THE PATENTS RULE, 2003
COMPLETE SPECIFICATION
[See section 10, rule 13]
AN IMPROVED PROCESS FOR PREPARATION OF SARPOGRELATE AND ITS SALT
APPLICANT:
CALYX CHEMICALS AND PHARMACEUTICALS LTD. 2, Marwah's Complex, Sakivihar Road, Sakinaka, Andheri (E), Mumbai-400 072, Maharashtra, India
Indian Company incorporated under the Companies Act 1956
The following specification particularly describes the invention and the manner in which it is to be performed:

FIELD OF THE INVENTION
The present invention in general relates to a simple and eco-friendly process for preparing Sarpogrelate. More particularly, the present invention relates to an improved process for preparation of Sarpogrelate and its salts employing water as a solvent.
BACKGROUND OF THE INVENTION
4-[2-(Dimethylamino)-l-({2-[2-(3-methoxyphenyl) ethyl] phenoxy} methyl) ethoxy]-4-oxobutanoic acid of Formula I, commonly known as Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. It blocks serotonin-induced platelet aggregation, and has applications in the treatment of many diseases including diabetes mellitus, Buerger's disease, Raynaud's disease, coronary artery disease, angina pectoris and atherosclerosis.

Sarpogrelate was first disclosed in US4485258 wherein the process for preparation of Sarpogrelate is also disclosed. The process for preparation of Sarpogrelate involves reaction of pure 2-(3-Methoxyphenethyl) phenol with epichlorohydrin to obtain epoxide in presence of organic solvent like N,N-dimethylformamide. The epoxide

formed is allowed to react with amine and on further reaction with acid anhydride, Sarpogrelate is formed. Both the later steps of the reaction are carried out in presence of organic solvent like tetrahydrofuran.
J. Med. Chem. 1990, Vol. 33, 1823-1827 describes the process for preparation of
[2[(aminoalkoxy)phenyl]ethyI] benzenes. The preparation of
[2[(aminoalkoxy)phenyI]ethyI] benzenes is exemplified by preparation of [2-(Dimethylamino)-l-[[2-(2-pheynylethyl)-phenoxy-methyl]ehtyl]succinate hydrochloride. The process involves a] reaction of benzyl chloride with triphenyl phosphine in acetonitrile to obtain phosphonium salt, b] phosphonium salt is then treated with salicylaldehyde in presence of DBU and acetonitrile to yield stilbene compound which is hydrogenated with 5% Pd/C in ethanol to obtain 2-phenyl ethyl phenol, c] phenol compound is then reacted with epichlorhydrin in presence of NaH and DMF to get epoxide compound d] epoxide compound is then treated with 50% aqueous dimethyl amine in THF to get dimethylamino compound which is treated with succininc anhydride in acetone to get final exemplified compound e] final compound is then converted to its hydrochloride salt by reacting with 20% HC1 in ethyl acetate. The articles reports that among compounds studied, Sarpogrelate was taken for the further biologic studies.
J. Med. Chem. 2006, Vol. 49 (22), 6607-6613 discloses the process for preparation of 2-(3-Methoxyphenethyl) phenol by hydrogenation of 2-(3-Methoxystyryl) phenol which in turn is prepared through Wittig's reaction. The hydrogenation step of the reaction is carried out in organic solvent selected from alcohols. The Wittig's reaction is carried out in solvent like acetonitrile. The process disclosed also involves purification of 2-(3-Methoxyphenethyl) phenol by column chromatography.
The above discussed processes involve use of organic solvents for each of the step thereby making the process costlier and harmful to the environment. The problems

associated with the above prior art can be overcome by using commercially viable and eco-friendly process and solvents.
Organic reactions that proceed in aqueous medium without the use of organic solvents have been attracting attention from the viewpoint of environmental care. However, various disadvantages existed for the use of aqueous medium for organic reactions, causing the procedure to be considered difficult. The first main disadvantage is that organic compounds are mostly insoluble in water; the second disadvantage is that most reaction intermediates and reagents such as catalysts are decomposed by even a trace of water.
However, the inventors of the present invention have rationally designed an improved process for preparation of Sarpogrelate in water making the process eco-friendly, inexpensive and industrially viable. Also the product obtained is in high yield and high purity without involving tedious and costlier purification processes like column chromatography.
OBJECT OF THE INVENTION
a) An object of the present invention is to provide an improved process for the preparation of Sarpogrelate from 3-methoxy benzyl halide.
b) Another object of the present invention is to provide an improved process for the preparation of Sarpogrelate by in-situ preparation of phosphonium salt of Formula IV
c) Another object of the present invention is to provide improved processes for the preparation of Sarpogrelate wherein water is used as a solvent.

d) Yet another object of the present invention is to provide simple, economic, eco-friendly and industrially viable processes for the preparation of Sarpogrelate.
e) Yet another object of the present invention is to provide simple, economic, eco-friendly and industrially viable processes for the preparation of Sarpogrelate hydrochloride.
SUMMARY OF THE INVENTION
comprising
a) reacting 3-methoxy benzyl halide of Formula HI

According to an aspect of the present invention, there is provided an improved process for preparation of Sarpogrelate of Formula I and its salts,


wherein, X is halide
with triphenylphosphine in presence of water as a solvent to obtain compound of Formula IV

b) reacting compound of Formula IV with salicylaldehyde in presence of a base and water as a solvent to obtain compound of Formula V

c) purifying compound of Formula V utilizing an alcohol and cobalt (IT) chloride
d) hydrogenating the purified form of compound of Formula V in presence of an aqueous base and a transition metal catalyst under hydrogen pressure to obtain a compound of Formula VI

e) reacting compound of Formula VI with epichlorohydrin using a base and in absence of any solvent to obtain an epoxide of Formula VII


f) reacting the epoxide of Formula VII with aqueous dimethylamine to obtain compound of Formula VIII

g) reacting the compound of Formula VIII with succinic anhydride in presence of an organic solvent to obtain Sarpogrelate base
In another aspect of the present invention, there is provided an improved process for the preparation of Sarpogrelate hydrochloride of Formula II, comprising,


reacting Sarpogrelate base of Formula I obtained in step g), as described above with hydrochloride source in alcoholic solvent, optionally, followed by purification utilizing lower aliphatic ketone like acetone.
In another aspect of the present invention there is provided an improved process for preparation of Sarpogrelate of Formula I and its salts, by in-situ preparation of phosphonium salt of Formula IV, comprising, i) reacting 3-methoxy benzyl halide of Formula HI

wherein, X is halide
with triphenylphosphine in presence of water as a solvent followed by reacting
with salicylaldehyde in presence of a base to obtain compound of Formula V

ii) converting compound of Formula V to Sarpogrelate of Formula I by following the process of step c) to step g), as described herein above.

DETAILED DESCRIPTION OF THE INVENTION
Nowadays with increasing ecological problems like pollution, global wanning etc., the emphasis in industries is not only on economical process but also on green processes. Thus, in present circumstances it has become a need to combine economic and ecological principle in any process development. Accordingly, these objects are accomplished by the present invention, which in its broadest aspects provides an improved process for preparation of Sarpogrelate and its salts without utilizing hazardous solvents as well as high capital intensive and operationally unfriendly process.
The present invention relates to the improved, simple and eco-friendly process for the preparation of Sarpogrelate of Formula I and its salts

The present invention also relates to an improved process for the preparation of Sarpogrelate Hydrochloride of Formula II


The process of the present invention for the synthesis of Sarpogrelate and its salt is as shown in the Scheme I below

SCHEME I


In an aspect of the present invention there is provided an improved process for
preparation of Sarpogrelate of Formula I and its salts,
comprising
a) reacting 3-methoxy benzyl halide, compound of Formula HI

wherein, X is halide
with triphenylphosphine in presence of water as a solvent to obtain compound of
Formula IV


c) purifying compound of Formula V utilizing an alcohol and cobalt (II) chloride
b) reacting compound of Formula IV with salicylaldehyde in presence of a base and water as a solvent to obtain compound of Formula V

d) hydrogenating the purified form of compound of Formula V in presence of an aqueous base and a transition metal catalyst under hydrogen pressure to obtain a compound of Formula VI

e) reacting compound of Formula VI with epichlorohydrin using a base in absence of any solvent to obtain an epoxide of Formula VII

f) reacting the epoxide of Formula VII with aqueous dimethylamine to obtain compound of Formula VIII

g) reacting the compound of Formula VTH with succinic anhydride in presence of an organic solvent to obtain Sarpogrelate base.

In another aspect of the present invention there is provided an improved process for preparation of Sarpogrelate of Formula I and its salts, by in-situ preparation of phosphonium salt of Formula IV, comprising, i) reacting 3-methoxy benzyl halide of Formula III

wherein, X is halide
with triphenylphosphine in presence of water as a solvent followed by reacting
with salicylaldehyde in presence of a base to obtain compound of Formula V

ii) converting compound of Formula V to Sarpogrelate of Formula I by following the process of step c) to step g), as descirbed herein above.
In an embodiment of the present invention, step a), step b), step d) and step f) are carried out in presence of water as a solvent where as step e) is carried out without using any solvent. Thus, process of present invention is simple, eco-friendly and cost effective over known prior art processes.
In step g), compound of Formula VIII is converted to Sarpogrelate using succinic anhydride in presence of organic solvent by known prior art process.

In another embodiment of the present invention, alternately Sarpogrelate is prepared by in-situ preparation of phosphonium salt of Formula IV. Compound of Formula V is prepared from 3-methoxy benzyl halide of Formula III without isolating compound of Formula IV. Thus, process of present invention avoids isolation of compound of Formula TV and minimizes the use of solvent.
According to another embodiment of the present invention, the molar ratio of the triphenylphosphine with respect to compound of Formula HI is in the range of 0.5 to 2, preferably it is 0.9 to 1.5
According to another embodiment of the present invention, the molar ratio of salicylaldehyde with respect to compound of Formula III is in range of 0.5 to 2, preferably in range of 0.8 to 1.1.
The base used in step b) and step i) is selected from alkali metal hydroxides or alkali metal carbonates, wherein the alkali metal hydroxides such as sodium hydroxide, potassium hydroxides are used and the alkali metal carbonates such as potassium carbonate, sodium carbonate are used.
The molar ratio of the base used, with respect to compound of Formula HI is in range of 0.5 to 1.5, preferably it is 0.9 to 1.3.
The step a), step b) and step i) of the present invention is carried out at temperature ranging from 75°C to 110°C, preferably from 90°C to 100°C for 2 to 10 hours, preferably for about 2 to 8 hours.
According to further embodiment of the present invention, the compound of Formula V is purified utilizing alcohol and cobalt (II) chloride.

The alcohol used is selected from methanol, ethanol, propanol, isopropyl alcohol and the like.
The molar ratio of the cobalt (II) chloride used, with respect to compound of Formula HI is in the range of 0.5 to 2, preferably it is 0.9 to 1.1
According to yet another embodiment of the present invention, the aqueous base used in step d) is selected from alkali metal hydroxides like sodium hydroxide, potassium hydroxide.
The molar ratio of the base used for preparing aqueous base, with respect to compound of Formula V is in range of 0.5 to 3, preferably it is 1 to 2.
The amount of water used for preparing aqueous base, is in the range of 2 to 10 volumes with respect to compound of Formula V.
The transition metal catalyst used in step d) is selected from palladium, platinum, rhodium, or nickel. The catalyst is supported or unsupported. Preferably 5 to 10 % palladium on carbon is used.
The amount of catalyst used with respect to compound of Formula V is in the range of 5 to 12 % wt/wt.
The hydrogenation step is carried out under hydrogen pressure ranging from 3 to 20 Kg/cm2 , preferably from 5 to 12 Kg/cm2 .
The hydrogenation step is carried out at temperature of 25 to 100°C, preferably at 40 to 70°C.

According to yet another embodiment of the present invention, the base used in step e) is selected from alkali metal hydroxides like sodium hydroxide, potassium hydroxide
The molar ratio of the base used with respect to compound of Formula VI is in range of 1 to 5.
The molar ratio of the epichlorohydrin used with respect to compound of Formula VI is in range of 1 to 5.
The step e) of the present invention is carried out at temperature of 30 to 100°C, preferably 50 to 80°C for 1 to 10 hours, preferably 2 to 5 hours.
According to yet another embodiment of the present invention, the molar ratio of dimethylamine used in step f) with respect to compound of Formula VII, ranges from 1 to 6.
The step f) of the reaction is carried out at temperature of 25 to 60°C, preferably at 40 to 50°C for 0.5 to 6 hours.
According to yet another embodiment of the present invention, the molar ratio of succinic anhydride used in step g) with respect to compound of Formula VIII is in the range of 1 to 5, preferably 1 to 3.
The step g) of the reaction is carried out in presence of organic solvent like acetone, methylene dichloride, acetonitrile, ethyl acetate, tetrahydrofuran and the like, preferably acetone.

The step g) of the reaction is carried out at temperature of 30 to 100°C, preferably 50 to 70°C for 1 to 5 hours, preferably 2 to 3 hours.
In another aspect of the present invention, there is provided an improved process for the preparation of Sarpogrelate hydrochloride of compound of Formula II comprising, reacting Sarpogrelate base of Formula I with hydrochloride source in alcoholic solvent, optionally, followed by purification utilizing lower aliphatic ketone like acetone.
The hydrochloride source can be hydrochloric acid or hydrogen chloride gas dissolved in alcoholic solvents like isopropyl alcohol.
The details of the invention provided in the following example are given by the way of illustration only and should not be construed to limit the scope of the present invention.
EXAMPLES
Example 1
Preparation of (3-Methoxvbenzyl)triphenyl phosphonium chloride (Formula
IV) from 3-methoxybenzyl chloride (Formula III)
To 200ml of water was added to 175gms of triphenylphosphine and the mixture was stirred for 5 minutes. To the mixture was then added 100gms of 3-methoxybenzyl chloride and 100ml of water. The mixture was stirred for 15 minutes and heated slowly to reach reflux temperature. The mixture was maintained at 95°C for 3 hours. The water in mixture was distilled off under vacuum. To the mixture was then added 100ml of toluene which was degassed completely. Further the degassed mass was re-slurried with 350 ml of toluene and the mixture was heated to 85-90°C this temperature was further maintained for 1

hour. The mixture was then cooled to room temperature and filtered. The solid cake obtained was washed with toluene and dried at 45-50°C to obtain 238gms of (3-Methoxybenzyl)triphenyl phosphonium chloride Yield: 88.93%
Example 2
Preparation of 2-(3-MethoxYstvryl)phenol (Formula V) from (3-
Methoxybenzyl)triphenyl phosphonium chloride (Formula IV)
To 100ml of water was added 50gms of (3-Methoxybenzyl)triphenyl phosphonium chloride (Formula IV) with stirring and the stirring was continued for 10 minutes. To this mixture was then added 11gms of sodium bicarbonate and the mixture was slowly heated for 0.5 hours at 65-70°C. To the reaction mixture was added 14.56gms of salicyaldehyde slowly. Formation of yellow colored solution was observed. The reaction mixture was further heated to 90-92°C and the temperature was maintained for 7 hours. After completion of reaction 700ml of toluene was added and was stirred for 0,5 hours at room temperature. The organic and aqueous layers were separated and the aqueous layer was extracted again with 200ml (2X 100ml) of toluene. The organic layers were combined and washed with 100ml (2 X 50ml) of IN hydrochloric acid. The mixture was stirred for 0.5 hours at 25-30°C and the organic layer was separated and washed with 280ml (70ml X 4) of water till the pH is neutral. The organic layer was then separated and toluene was distilled out under vacuum at 50-55°C to obtain 70gms of crude 2-(3-Methoxystyryl) phenol.

Example 3
Preparation of 2-(3-MethoxYStyryl) phenol (Formula V) from 3-methoxvbenzyl chloride (Formula IIP Hn-situ preparation of phosphonium salt of Formula IVI
To 500ml of water was added to lOOgms of 3-methoxybenzyl chloride and 158.7gms of triphenylphosphine. The mixture was stirred and heated slowly to reach 95-100°C temperature. The mixture was continued to be heated at 95-100°C for 3 hours. After completion of reaction (checked by TLC), the reaction mixture was cooled to 65-70°C, 58.95gms of sodium bicarbonate was slowly added in 0.5 hours at 65-70°C. The reaction mixture was stirred for another 0.5 hours and then 77,8gms of salicyaldehyde was slowly added in 0.5 hours. Formation of yellow colored solution was observed. The reaction mixture was further slowly heated to 95-100°C and the temperature was maintained for 4 hours. After completion of reaction (checked by TLC), 700ml of ethyl acetate was added and was stirred for 0.5 hours at room temperature. The organic and aqueous layers were separated and the aqueous layer was extracted again with 100ml of ethyl acetate. The organic layers were combined and washed with 100ml of IN hydrochloric acid. The mixture was stirred for 0.5 hours at 25-30°C and the organic layer was separated and washed with 800ml (200ml X 4) of water till the pH is neutral. The organic layer was further washed with 200ml of brine solution. The organic layer was then dried over sodium sulphate and distilled under vacuum at 45-50°C to obtain 333gms of crude 2-(3-Methoxystyryl) phenol.
Example 4: Purification of crude 2-(3-Methoxystryl) phenol
The crude 2:(3-Methoxystyryl) phenol obtained in Example 2 or 3 was taken in amount of 333gms and was dissolved in 500ml of methanol at 25-30°C to obtain clear solution. To this solution was added 163.99gms of cobalt (II) chloride and

the mixture was slowly heated to reflux at 65-70°C. The temperature was maintained for 2 hours. The mixture was then cooled to 0°C and was maintained for another 1 hour at same temperature. The mixture was then filtered and the solid cake obtained was washed with 50ml of methanol. The filtrate obtained was distilled under vacuum and degassed completely. To the degassed mass was added 500ml of ethyl acetate and the mixture was stirred for 0.5 hours to make slurry. The mixture was filtered and the solid cake was washed with 200ml of ethyl acetate. The filtrate was collected and washed with 250ml of brine solution. The organic layer was further washed with 200ml (100ml X 2) of 15% sodium bisulphite. The organic layer was then added to 250ml of brine solution and the pH was adjusted to 6-7 using saturated sodium bicarbonate solution. The organic layer was separated and again washed with 250ml brine solution and dried over sodium sulphate. Solvent was distilled out under vacuum at 45-50°C to obtain 143gms of pure2-(3-Methoxystyryl) phenol. Yield: 99.30%
Example 5
Preparation of 2-(3-Methoxvphenethyl)phenol (Formula VI)
To the solution of 37.96gms of sodium hydroxide in 715ml of water was added 143gms of pure 2-(3-Methoxystyryl) phenol obtained in Example 4 at 25-30°C. The aqueous layer was washed with 600ml (200ml X 3) of 5% ethyl acetate in hexane. The aqueous solution was then taken in a clean autoclave and 10.8gms of 10% Pd/C was added to it. The autoclave was flushed with nitrogen once under stirring and then flushed with hydrogen once. 10kg hydrogen pressure was provided and the reaction mixture was heated to 60°C, these reaction conditions were maintained for 2-3 hours. After completion of the reaction (checked by TLC), the reaction mixture was cooled to 25-30°C and filtered to recover Pd/C. The filtrate obtained was again filtered through hy-flow and the hy-flow bed was

washed with 150ml of ethyl acetate. The pH of mother liquor was adjusted to 4-5 using 30% conc. HC1. To the mixture was then added 150ml of ethyl acetate and stirred for 0.5 hours. The layers were then separated and the aqueous layer was again extracted with 150ml of ethyl acetate. The organic layers were combined and washed with 300ml of water followed by washing with 300ml of brine solution. The organic layer was then dried over sodium sulphate and distilled under vacuum at 50-55°C to obtain 129gms of 2-(3-Methoxyphenethyl)phenol. Yield: 89.45 %
Example 6
Preparation of 2-(Y2-(3-MethoxvphenethvnphenoxvV methyl)oxirane
(Formula VIII)
To 129gms of 2-(3-Methoxyphenethyl) phenol obtained in Example 5 was added 45.23gms of sodium hydroxide with vigorous stirring and was further stirred for 0.5 hours. To the stirred mixture was then added 104.67gms of epichlorohydrin (exotherm was observed) and was further stirred for 0.5 hours. The reaction mixture was heated to 65-70°C and then maintained for 2.5 hours. After the completion of the reaction (TLC checked), the reaction mixture was cooled to 25-30°C and 390ml of ethyl acetate and 520ml of water was added. The mixture was stirred for 0.5 hours and was filtered through hy-flow bed. The hy-flow bed was washed with 260ml (2 X 130ml) of ethyl acetate. The organic layer was separated and the aqueous layer was extracted with 130ml of ethyl acetate. The organic layers were combined and washed with 260ml of saturated sodium bicarbonate solution. The combined organic layer was then washed with 260ml of brine solution and distilled under vacuum at 50-55°C to obtain 148gms of 2-((2-(3-Methoxyphenethyl)phenoxy)- methyl)oxirane. Yield: 92.10%

Example 7
Preparation of l-(2-(3-Methoxvphenethyl)phenoxv)-3-(dimethvlamino)
propan -2-ol (Formula VIII)
To 148gms of 2-((2-(3-Methoxyphenethyl)phenoxy)- methyl)oxirane obtained in Example 4 was added 234.5gms of 40% dimethylamine at 30°C. The reaction mixture was then stirred at room temperature for 4 hour. After completion of reaction (TLC checked), the lower oily mass was separated and the aqueous layer was extracted with 148 ml of ethyl acetate. The ethyl acetate extract was combined with oily mass and again 296 ml of ethyl acetate was added to it. The organic layer obtained was washed with 296 ml of water and followed by washing with 296ml of brine solution. The organic layer then was dried over sodium sulphate and distilled under vacuum at 45-50°C to obtain 157 gms of 1-(2-(3 -MethoxyphenethyI)phenoxy)-3 -(dimethylamino)propan-2-ol. Yield: 91.57%
Example 8
Preparation of 4-(3-(2-(-3-Methoxyphenethyl)phenoxy)-l-dimethylamino)
propan-2-yloxy)-4-oxo-butanoic acid (Sarpogrelate hydrochloride)
To the 157gms of l-(2-(3-Methoxyphenethyl)phenoxy)-3-
(dimethylamino)propan-2-ol was added 392ml of acetone at 30°C and the mixture was stirred for 10mins. Further to this mixture were added 95.44gms of succinic anhydride and 78ml of acetone. The reaction mixture obtained was heated slowly to reflux and the mixture was maintained at 55-60°C for 2 hours. After completion of reaction (TLC checked), the reaction mixture was cooled and filtered. The filtrate was cooled to 0-5°C and slowly drop-wise 95.8gms of 20% isopropyl alcohol hydrochloride was added with stirring. The solid obtained was filtered and the solid cake was washed with 314ml (157ml X 2) of acetone. The

solid was dried under vacuum at 50-55°C to get 158gms of crude Sarpogrelate
salt.
Yield: 71.05%
Example 9: Purification of Sarpogrelate hydrochloride
The crude product obtained in Example 8 was dissolved in 474ml of acetone at 25-30°C and slowly heated to reflux. The temperature was maintained at 55-60°C for 1 hour and then cooled to 40-45°C. The solid obtained was filtered and washed with 158ml of acetone. The product was dried at 50-55°C for 6 hours to obtain 153.8gms of pure Sarpogrelate hydrochloride, Yield: 69.13%

We claim
1. An improved process for preparation of Sarpogrelate of Formula I and its salts,

comprising,
a) reacting 3-methoxy benzyl halide, compound of Formula in

wherein, X is halide,
with triphenylphosphine in presence of water as a solvent to obtain compound of
Formula IV

b) reacting compound of Formula IV with salicylaldehyde in presence of a base and water as a solvent to obtain compound of Formula V


c) purifying compound of Formula V utilizing an alcohol and cobalt (II) chloride
d) hydrogenating the purified form of compound of Formula V in presence of an aqueous base and a transition metal catalyst under hydrogen pressure to obtain a compound of Formula VI

e) reacting compound of Formula VI with epichlorohydrin using a base in absence of any solvent to obtain an epoxide of Formula VII

f) reacting the epoxide of Formula VII with aqueous dimethylamine to obtain compound of Formula VIII


g) reacting the compound of Formula VIII with succinic anhydride in presence of an organic solvent to obtain Sarpogrelate base
2. An improved process for preparation of Sarpogrelate of Formula I and its salts, by in-situ preparation of triphenylphosphonium salt of Formula IV,

Formula I
comprising,
i) reacting 3-methoxy benzyl halide of Formula HI

wherein, X is halide

with triphenylphosphine in presence of water as a solvent followed by reacting with salicylaldehyde in presence of a base to obtain compound of Formula V

ii) purifying compound of Formula V utilizing an alcohol and cobalt (II) chloride iii) hydrogenating the purified form of compound of Formula V in presence of an
aqueous base and a transition metal catalyst under hydrogen pressure to obtain
a compound of Formula VI

iv) reacting compound of Formula VI with epichlorohydrin using a base in absence of any solvent to obtain an epoxide of Formula VII

v) reacting the epoxide of Formula VII with aqueous dimethylamine to obtain compound of Formula VIII


vi) reacting the compound of Formula VIII with succinic anhydride in presence of an organic solvent to obtain Sarpogrelate base
3. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, wherein the step a), step b) and step i) is carried out at temperature ranging from 75°C to 110°C, preferably from 90°C to 100°C for 2 to 10 hours, preferably for about 2 to 8 hours
4. The process for preparation of Sarpogrelate as claimed in claim I or 2, wherein in the base used in step b) and step i) is selected from alkali metal hydroxides or alkali metal carbonates, wherein the alkali metal hydroxides such as sodium hydroxide, potassium hydroxides are used and the alkali metal carbonates such as potassium carbonate, sodium carbonate are used
5. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, wherein in the base used in hydrogenation and epoxide formation step is selected from alkali metal hydroxides like sodium hydroxide, potassium hydroxide
6. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, wherein in hydrogenation is carried out under hydrogen pressure ranging from 0.5 to 20 Kg/cm , preferably from 5 tol2 Kg/cm2 at temperature range of 25 to 100°C, preferably at 40 to 70°C

7. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, wherein in the step e) and step iv) the molar ratio of the epichlorohydrin used with respect to compound of Formula VI is in range of 1 to 5
8. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, wherein the step e) and step iv) is carried out at temperature of 30 to 100°C, preferably 50 to 80°C for 1 to 10 hours, preferably 2 to 5 hours
9. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, wherein the step f) and step v) is carried out at temperature of 25 to 60°C, preferably at 40 to 50QC for 0.5 to 6 hours
10. The process for preparation of Sarpogrelate as claimed in claim 1 or 2, further comprises formation of hydrochloride salt of Sarpogrelate by reacting Sarpogrelate base with hydrochloride source in presence of alcoholic solvent like isopropyl alcohol, optionally, followed by purification utilizing lower aliphatic ketone like acetone.