Disclosed is a process for preparation of (3S)-3-[4-[(5-halo-2-chlorophenyl) methyl] phenoxy] tetrahydrofuran of Formula 1. The process comprises condensing 4-[(5-halo-2-chloro-phenyl)methyl]phenol of Formula 2 with [(3R)-tetrahydrofuran-3-yl]benzenesulfonate derivative of Formula 3 in the presence of a base and sol...
Disclosed is an improved process for preparation of a Clocortolone Pivalate of formula (I) and polymorphic form A thereof. The process of the present invention is a multi step process where the starting material is 17-desoxy steroid. The process of the present invention comprises reacting a 9,11-epoxy compound of fo...
The present invention provides a process for preparation of 6α-fluoro-9β,11β-epoxy-pregna-
1,4,16-triene-3,20-dione-21 -acetate of formula (A), which process includes:
a) reacting 9β,11β-epoxy-pregna-1,4,16-triene-3,20-dione-21-acetate of formula (I) with an acylating agent to yield 21-(acetyloxy)-9β,11β-epoxy-pre...
The present invention provides a stereo-specific synthesis of Moxifloxacin intermediate (4aS,7aS)-2,3,4,4a,5,6,7,7a-octahydro-lH-pyrrolo[3,4-b]pyridine of formula (A), which comprises resolution of cis compound 6-benzyl-l,2,3,4,4a,7a-hexahydropyrrolo[3,4-b]pyridine-5,7-dione of formula (1) using D(-)-tartaric acid. ...
Abstract
PROCESS FOR PREPARATION OF N-BENZYL-3-HYDROXY PIPERIDINE
Disclosed is a process for preparation of N-benzyl-3-hydroxy piperidine of Formula 1. The process comprises reacting 3-hydroxy pyridine of Formula 2 with benzyl halide of Formula 3 in the presence of hydrocarbon solvents to form 1-benzyl-3-hydro...
Disclosed is an improved process for preparation of arylboronic acid of Formula 1. The process comprises reacting aryliodide substituted by an electrophillic functional group of Formula 2 with alkyl magnesium halide in the presence of a hydrocarbon solvent to form Grignard species of Formula 3. Further, Grignard spe...
The present invention provides a process for preparing l-[3-[(E)-2-(7-chloro-2-quinoryl)vinyl]phenyl]ethanone of formula (A), which comprises condensation of 7-chloro-2-methyl-quinoline of formula (I) with 3-acetylbenzaldehyde of formula (II). The process is schematically represented as shown in Scheme-1 below-
S...
Process for preparation of (R)-([(adenine-9-yl)-propan-2-oxy]-methyl)-phosphonic acid and hydrates thereof
Described is a process for the preparation of a compound of formula (A) and hydrates thereof.
The present invention relates to process for preparing triazole compounds used in the treatment of epilepsy. The process comprises of reacting compound of 2, 6 difluoroazide (II) with 2, 3 dihalo compound (III) to form compound of formula I, which on further treatment with an aminating agent gives Rufinamide (IV). 2...
ABSTRACT
Process For Synthesis Of Intermediates Of Nilotinib And Nilotinib
The present invention discloses a process to prepare nilotinib and pharmaceutically acceptable salts, particularly the invention discloses a process to prepare an intermediate of nilotinib of formula (A).
The present invention provides a stereo-specific synthesis of Moxifloxacin intermediate (4aS,7aS)-2,3,4,4a,5,6,7,7a-octahydro-lH-pyrrolo[3,4-b]pyridine of Formula (A) from (4aR,7aS)-6-benzyl-1,2,3,4,4a,7a-hexahydropyrrolo[3,4-b]pyridine-5,7-dione of Formula (II) comprising resolution of cis compound 6-benzyl-l,2,3,4...
The present invention relates to an improved process for the preparation of Acalabrutinib intermediates (3-chloropyrazin-2-yl) methanamine and acid salt thereof and 2-((3-chloropyrazin-2-yl)methylcarbamoyl) pyrrolidine-1-carboxylic acid ester that is cost effective and gives higher yield and better purity.
...
The present invention provides a stereo-specific synthesis of Moxifloxacin intermediate (4aS,7aS)-2,3,4,4a,5,6,7,7a-octahydro-lH-pyrrolo[3,4-b]pyridine of formula (A), which comprises resolution of cis compound 6-benzyl-l,2,3,4,4a,7a-hexahydropyrrolo[3,4-b]pyridine-5,7-dione of formula (1) using D(-)-tartaric acid. ...
Provided herein is an improved process for the preparation of 1H-pyrrolo[2,3-b]pyridin-5-ol, which is useful in the preparation of a key intermediate of Venetoclax. Said process increases the % yield of intermediates by about 96% to 99%.
10
Provided herein is a process for the preparation of a 4-halo-2-alkoxy-5-nitroaniline, and more particularly to a process for preparation of 4-halo-2-methoxy-5-nitroaniline being cost effective with higher yield, higher HPLC purity and minimizing isomeric impurities formation.
Improved process for preparation of 1-(3-methyl-1- phenyl-1H-pyrazol-5-yl)piperazine
Disclosed is a process for preparation of 1-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazine of Formula I. The process comprises reacting N-protected derivative of 1-piperazin-1-ylbutane-1,3-dione of Formula II with phenyl hydrazine o...
“PROCESS FOR PREPARATION OF 1-[3-[(E)-2-(7-CHLORO-2-QUINOLYL) VINYL] PHENYL] ETHANONE”
The present invention provides a process for preparing 1-[3-[(E)-2-(7-chloro-2-quinolyl)vinyl]phenyl]ethanone of formula (A), which comprises condensation of 7-chloro-2-methyl-quinoline of formula (I) with 3-acetylbenzaldehyde of...
Provided herein is a process for the preparation of a novel [4-cyano-3-(trifluoromethyl)phenyl]carbamodithioic acid and its use in preparation of Enzalutamide being cost effective with higher yield, higher HPLC purity with reduced impurities.
Provided herein is an improved process for the preparation of alkyl 3-amino-5-bromo-2-methyl-benzoate, which is useful in the preparation of a key intermediate of Tazemetostat. Said process increases the % yield of intermediates by about 96% to 99%.
Provided herein is a process for the preparation of Empagliflozin and its (R)-isomer or salts thereof, wherein Empagliflozin achieved is of with higher yield and higher chiral and HPLC purity. The process provides simple reaction work up for isolation of Empagliflozin or its (R)-isomer or its salts.
...
Provided herein is an improved process for the preparation of benzylated derivative of D-galactose, particularly 2,3,4,6-tetra-O-benzyl-D-galactose that gives higher yield and better purity being cost effective with reduced impurities.
Provided herein is a process for the preparation of a novel intermediate 1-[5-(2,4-difluorophenyl)-2-alkoxy-phenyl]ethanone and its use in preparation of Diflunisal being cost effective with higher yield, higher HPLC purity and better quality of Diflunisal. The process for synthesis of Diflunisal using novel interme...
The present invention discloses a process to prepare nintedanib and pharmaceutically acceptable salts thereof. The process comprises of reacting compound of Formula (II) and (III) to form compound of formula (IV), which on heating in the presence of a solvent forms nintedanib of Formula (I).
Provided herein is an improved process for preparation of alkali metal salt of 2,4-Dichlorophenoxy acetic acid of Formula (I) comprising forming an alkali metal salt of 2,4-dichlorophenol by adding 2,4-Dichlorophenol (2,4-DCP) and alkali metal hydroxide, followed by forming in situ alkali metal salt of monochloroace...
Provided herein is a process for preparing (3R)-hydroxy tetrahydrofuran with high enantiomeric excess comprising reacting (S)-sulfonyloxy derivative of tetrahydrofuran with a primary alcohol, secondary alcohol or a benzoyl derivative in presence of suitable base to form corresponding benzyl ether or benzoyl ester de...
Provided herein is an improved process for preparation of Deferasirox with reduced genotoxic impurities less than 0.5 ppm and with improved physical characteristics like colour.
Provided herein is a process for the preparation phenylboronic acid and its ester derivatives, and particularly carboxyphenyl boronic acid and its ester derivatives with lesser number of steps providing high yield and maximum HPLC purity and further obviating use of KMnO4 thereby forming less by-products and hence a...
ABSTRACT
PROCESS FOR PREPARATION OF 3-[4-[(2-CHLOROPHENYL)METHYL]PHENOXY] TETRAHYDROFURAN DERIVATIVES
Provided herein is a process for the preparation of process for preparation of 3-[4-[(2-chlorophenyl)methyl]phenoxy]tetrahydrofuran derivatives, avoiding impurity formation and thus yield loss and also increasin...
The invention relates to a process for preparation of sitagliptin (Formula (A)) and salts thereof, comprising, reacting a compound of Formula (I) with a first acid and a substituted alcohol having electron withdrawing groups.
The invention also relates to a process for preparation of compound of Formula (I...
Provided herein is a process for the preparation of specific enantiomeric Sitagliptin with good chiral purity and higher yield using improved biocatalyst and by engineering an enzyme to mediate the efficient conversion of ketoamide to obtain enantiomerically pure Sitagliptin in presence of an amino group donor.
...
Provided herein is a process for the preparation of alkyl or benzyl ester of [4-cyano-3-(trifluoromethyl)phenyl]carbamodithioic acid and its application thereof.
The present invention relates to a process for the preparation of l-bromo-2,4,5-trifluorobenzene from 2,4,5-trifhioroaniline or sulfate salt thereof. The present invention also relates to a process for the preparation of 1,2,4-trifluorobenzene from 2,4,5-trifluoroaniline and then converting into 1-bromo-2,4,5 -trifl...
Disclosed is a process for preparation of (3S)-3-[4-[(5-halo-2-chlorophenyl) methyl] phenoxy] tetrahydrofuran of Formula 1. The process comprises condensing 4-[(5-halo-2-chloro-phenyl)methyl]phenol of Formula 2 with [(3R)-tetrahydrofuran-3-yl]benzenesulfonate derivative of Formula 3 in the presence of a base and sol...
The present invention provides an improved process for synthesis of [tetrahydrofuran-3-yl]-4-methylbenzenesulfonate of formula (A), which comprises reaction of 3-tetrahydrofuran-ol with p-tosylchloride in the presence of an inorganic base selected from the group consisting of alkali hydroxides, alkali metal carbonat...
Provided herein is a process for the preparation of Apalutamide using a novel compound i.e. alkyl or benzyl ester of N-[6-cyano-5-(trifluoromethyl)-3-pyridyl]carbamodithioic acid and its preparation thereof, the process being cost effective with higher yield, higher HPLC purity with reduced impurities and without us...
Provided is a process for the preparation of umeclidinium bromide from a compound of formula (II). The process also provides a process for the preparation of compound of formula (II).
The present invention is related to a process for preparation of substituted pyrrolo[2,3-b]pyrazine compound Formula (I), an intermediate in the manufacturing of Upadacitinib.
The present invention discloses a novel, efficient and industrially advantageous process for the preparation of 2-chloro-4-methylaniline of formula I comprising chlorination of N protected toluidine of formula III to obtain N protected ortho chloro toluidine of formula II which is further deprotected to obtain 2-chl...
The present invention discloses a process for the preparation of 4'-(bromomethyl)[1,1'-biphenyl]- 2-carbonitrile of formula I from 4'-methyl-2-cyanobiphenyl of formula II with improved yield and purity involving the use of simple brominating reagent in a batch reactor.
Provided is process for the preparation of 4-amino-2-fluoro-N-methylbenzamide, an intermediate used in synthesizing enzalutamide and apalutamide. The process involves hydrogenation of 4-nitro-2-halo-N-methylbenz-amide of formula (II) in presence of bimetallic catalyst in a chemical reactor.
IMPROVED PROCESS FOR SYNTHESIS OF BENAZEPRIL INTERMEDIATE
The present invention relates to an improved process for the preparation for the stereo-specific preparation of Benazepril intermediate (3S)-3-[[(1S)-1-phenylethyl]amino]-1,3,4,5-tetrahydro-1-benzazepin-2-one of formula (IS). The steps include: heating the ...
The present invention relates to a process for the preparation of 2-chloro-4-fluorotoluene of formula I from diazotization of 2-chloro-4-aminotoluene of formula III.
The present invention relates to a process for the preparation of 2,3-dichloro-4-hydroxyaniline of formula I from 2,3-dichloronitrobenzene of formula III. The present invention also relates to a process for the purification of 2,3-dichloro-4-hydroxyaniline of formula I.
The present invention relates to a process for the preparation of 2-nitro-4-methylsulfonyl benzoic acid of formula I. The present invention also relates to a process for the purification of 2-nitro-4-methylsulfonyl benzoic acid of formula I.
The present invention discloses a process for hydrodechlorination of 2,5-dichlorotoluenes to obtain toluene and monochlorotoluenes. Particularly, the present invention discloses a process for hydrodechlorination of dichlorotoluenes, wherein the selectivity for toluene and 3-chlorotoluene is higher.
...
A PROCESS FOR THE PREPARATION OF 3-CHLORO-4-AMINO-5-NITROBENZOTRIFLUORIDE
The present invention discloses an industrially feasible and environmentally friendly process for the preparation of 3-chloro-4-amino-5-nitrobenzotrifluoride (Formula I) from 4-amino-3-nitrobenzotrifluoride (Formula II). Further, the present ...
The present invention discloses a process for the preparation of benzonitrile compounds of Formula (I) from the corresponding benzotrichloride compounds of Formula (II).