Abstract: The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.

Abstract: This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide.

Abstract: This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide.

Abstract: Disclosed herein is an improved process for the preparation of (R)-(+)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide (Brinzolamide) and novel intermediates thereof.

Abstract: A process for preparation of imiquimod comprising oxidation of 1-Isobutyl-1H-imidazo quinoline quinoline (II) afforded 1-Isobutyl-1H-imidazo-[4,5-c]-quinoline-5-N-oxide (III) which is isolated in pure form as its hydrochloride salt (IV) followed by conversion to 4-chloro derivative (V) and conversion to corresponding 4-iodo derivative (VI) which is a new intermediate. This new intermediate is convened to imiquimod (VIII) and purified via its novel maleate salt.

Abstract: The present invention discloses a novel process for preparation of carvedilol by using eco friendly solvents to obtain the said carvedilol in high purity. The said process comprises, reacting 4-hydroxy carbazole of formula (IV) with epichlorhydrin in presence of an organic solvent and a base at temperatures between 10° C.-30° C.; further reacting the resultant 4-(2,3-epoxypropoxy)- carbazole of formula (II) with a salt of 2-(2-methoxyphenoxy)ethylamine of formula (III), preferably hydrochloride salt in presence of a base and a hydroxylic solvent at temperatures between 30° C.-90° C.

Abstract: The present invention discloses a novel, stable polymorph of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine hydrochloride commonly known as Donepezil hydrochloride. Further the present invention discloses a process for producing Donepezil HCl amorphous and its polymorph Form (VI).

Abstract: The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HCl and 4[-2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide (I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride usingS methanolic ammonia and glacial acetic acid to obtain highly pure Glimepiride Form I (I) having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.

Abstract: A process for the preparation of 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]phenyl methyl]thiazolidine-2,4-dione maleate (the compound of Formula VI) comprising the steps of Coupling 2-[N-methyl-N-(2-pyridyl)amino]ethanol (the compound of Formula I) and 4-fluorobenzaldehyde (the compound of Formula II) in N,N-dimethylformamide, isolating the coupled product 4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]benzaldehyde (the compound of Formula III), converting said isolated benzaldehyde compound of formula III) to 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]benzylidene]thiazolidine-2,4-dione (the compound of Formula IV) and purifying the same, reducing 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]benzylidene]thiazolidine-2,4-dione, by a novel reduction method for making 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]phenyl methyl]thiazolidine-2,4-dione (the compound of Formula V).

Abstract: The present invention relates to an improved process for the preparation of 5,6-dihydro-4-(S)-(ethylamino)-6-(S)methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide hydrochloride of formula (I) commonly known as Dorzolamide Hydrochloride useful as an agent to reduce intraoccular pressure by inhibiting carbonic anhydrase enzyme

Abstract: A process for making Clopidogrel Bisulfate Form I which comprises dissolving Clopidogrel Bisulfate Form II in a solublizing solvent at room temperature to form a solution; adding an anti-solvent to the said solution till turbid; stirring the said turbid solution; collecting the precipitated solid and drying the final solid product, form I.

Abstract: The present invention discloses a novel, stable polymorph of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methyl piperidine hydrochloride commonly known as Donepezil hydrochloride. Further the present invention discloses a process for producing Donepezil HCl amorphous and it's polymorph Form (VI).

Abstract: The present invention discloses a novel, stable polymorph of 1-benzyl-4[(5,6-dimethoxy-1-indanone)-2-yl]methyl piperidine hydrochloride commonly known as Donepezil hydrochloride. Further the present invention discloses a process for producing Donepezil HCl amorphous and its polymorph Form (VI).

Abstract: The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.

Abstract: The present invention relates to the oxalate salt of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methyl piperidine, commonly known as Donepezil, and its method of preparation.

Abstract: The present invention discloses a process for the preparation of 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]phenyl methyl]thiazolidine-2,4-dione maleate (VI) comprising the steps of Coupling 2-[N-methyl-N-(2-pyridyl)amino]ethanol (I) and 4-fluorobenzaldehyde (II) in N,N-dimethylformamide, isolating the coupled product 4[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]benzaldehyde (III), converting said isolated benzaldehyde compound (III) to 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]benzylidene]thiazolidine-2,4-dione (IV) and purifying the same, reducing 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]benzylidene]thiazolidine-2,4-dione, by a novel reduction method for making 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy]phenyl methyl]thiazolidine-2,4-dione (V).