(R,S)-Nicotine was resolved through diastereomeric salt formation using dibenzoyl-d- tartaric acid and dibenzoyl-l-tartaric acid to obtain enantiomerically pure (S)-nicotine and (R)-nicotine.
The present invention provides a method for preparing colorless sucralose, wherein 4,l",6"-trichloro-4,1",6" -trideoxy-galactosucrose-6-acetate containing colored impurities formed during chlorination of sucrose-6-acetate is treated with sodium hypochlorite where sodium hypochlorite acts both as a decolorizing agent...
Process for the Preparation of Pregabalin
The present invention provides a new enantioselective method of preparing (S)-3- (aminomethyl)-5-methylhexanoic acid, commonly known as pregabalin. The invention also provides new chiral intermediates useful in the production of pregabalin.
The resolution of racemic l-(4-methoxybenzyl)-octahydro-isoquinoline, a key intermediate in the synthesis of the antitussive agent dextromethorphan, is reported using (R)-2-(6-methoxy-2-naphthyl) propionic acid in good yields. The resolving agent and the undesired isomer of the octahydro- isoquinoline have been reco...
A process for (R,S)-nicotine is described. Condensation of 1-(but-1-enyl) pyrrolidin-2-one with nicotinic acid ester gave 1-(but-1-enyl)-3-nicotinoylpyrrolidin-2-one which on treatment with an acid and a base gave myosmine. Myosmine was converted to (R,S)-nicotine by reduction followed by N-methylation.
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Process for the Preparation of Advantame :
A novelprocess for the preparation of N-[N-[3-(3-hydroxy-4-methoxyphenyl)-propyl]-L-a-aspartyl]-L-phenylalanine-l-methyl ester is described. It comprises, reacting isovanillin or its derivative with vinyl acétate followed by reductive condensation with L-[a-aspartyl]-L-phe...
A novel process for the preparation of L-threo-dihydroxyphenylserine (Droxidopa) is described. It comprises of enantioselective hydrolysis of racemic (DL)-threo-N-acetyl-3-(3,4-methylenedioxyphenyl)-serine using commercially available L-amino acylase from Aspergillus sp.(EC 3.5.1.14) in the presence of cobalt ions, ...
Process for the Preparation of Vilazodone Hydrochloride and Its Polymorph
A crystalline vilazodone hydrochloride has been prepared by reacting vilazodone free base with trimethylsilyl chloride using isopropanol as the solvent.
The present invention relates to a process for the preparation of 2-butyl-3-[[2"-(1H-tetrazol-5-yl)[1,1"-biphenyl]-4-yl]-l,3-diazaspiro[4,4]non-1-en-4-one by reaction of the corresponding nitrile with sodium azide and piperazine or its acid salt.
This invention discloses Strontium Ranelate polymorph, designated as Form A, having characteristic powdered x-ray diffraction pattern and infrared spectrum with water content of 1.5 to 2.5% and a process for its preparation.
The present invention relates to a novel and improved process for the preparation of linagliptin, chemically known as (R)-8-(3-amino-piperidin-l-yl)-7-but-2-ynyl-3-methyl-l-(4-methyl-quinazolin-2-ylmethyl)-3, 7-dihydro-purine-2, 6-dione through novel intermediates using (3S)-l-(7-(but-2-ynyl)-3-methyl-l-((4-methylqu...
The present invention relates to an improved process for the preparation of (1S, 3S, 5S)-2-[2(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl) acetyl]-2-azabicyclo [3.1.0] hexane-3-carbonitrile and its intermediates.
Preparation of 2-(4-Bromophenyl)-2-Methylpropanoic Acid
Selective bromination of 2-methyl-2-phenylpropanoic acid in aqueous medium is described to obtain pure 2-(4-bromophenyl)-2-methylpropanoic acid, which is a useful key intermediate in the process of manufacturing pure fexofenadine.
Process for the Preparation of Rivaroxaban :
A novel process for the preparation of rivaroxaban is described which comprises reacting 4-{4-[(5S)-5-(aminomethyl)-2-oxo-l,3-oxazolidin-3-yl] phenyl}-morpho!in-3-one with 5-chIoro thiophene -2-carbonyl chloride using epoxides as non-basic acid scavengers in the presen...
4,1",6"-Trichloro-4,1",6"-trideoxy-galactosucrose-6-acetate undergoes transesterification with alcohols in the presence of catalytic amount of metal oxide to give 4,1",6"-trichloro-4,1",6"-trideoxy-galactosucrose (sucralose) and alkyl acetate. The alkyl acetate formed and the solvent are removed by evaporation and t...
The present invention relates to an improved process for the preparation of N-(4-fluorobenzyl)-N-(l-methy!piperidinyl)-N"-(4-(2-methylpropyloxy)-phenylmethyl carbamide (Formula 1), also known as Pimavanserin, with excellent yield and high degree of chemical purity.
Process for the Preparation of Methyl 5-((2,4-difluorobenzyl) carbamoyl) -l-(2,2-dimethoxyethyI)-3-methoxy-4-oxo-l,4-dihydropyridine -2-Carboxylate:
Methyl 5- ((2,4-difluorobenzyl) carbamoyl)-!- (2,2-dimethoxyethyl)-3-methoxy-4-oxo-l,4-dihydropyridine-2-carboxylate is an important intermediate for the preparation o...
A novel crystalline Mirabegron which is a solvate of pentan-3-one is described. It is characterized by IR, XRDand DSC spectrum. The process of its preparation comprises treating Mirabegron with pentan-3-one and spontaneously obtaining the solvate as crystalline solid. The NMR and HPLC analysis of the solvate shows t...
A process for the preparation of 4-iodo-3-nitrobenzamide free from the impurities formed due to nucleophilic substitution of the labile iodo group is disclosed.
The present invention relates to a process for the conversion of gabapentin hydrochloride into gabapentin polymorphic Forms II or III by use of gaseous alkylamine and the choice of a specific solvent.
This invention discloses a process for converting gabapentin acid salt to free gabapentin, where the salt is dissolved in an organic solvent in which both gabapentin acid salt and free gabapentin are soluble. The solution is treated with a powdered alkaline base to liberate free gabapentin which will remain in solut...
Present invention is related to a process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3- methyl-1H-Indole (formula-1, a useful intermediate for the synthesis of bazedoxifene) using 4-benzyloxy propiophenone and 4-benzyloxy phenyl hydrazine hydrochloride.
Enantiomerically pure L-tert-leucine and D-tert-leucine were prepared from (DL)-tert- leucine by diastereomeric salt formation using dibenzoyl-d-tartaric acid as the resolving agent.
A novel process for the preparation of Bazedoxifene acetate and intermediates there of
A novel process is described for the preparation of pharmaceutical useful compounds such as 1 -{4-[2-(azepan-1 –y1)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate of fo...
Strontium ranelate is prepared by reacting dicyclohexylammonium ranelate with strontium halide in an anhydrous solvent. Strontium ranelate thus obtained will have less than 3% moisture content.
A process for the preparation of -ionylideneacetaldehyde by oxidizing β-ionylidene ethanol using 2, 2, 6, 6-tetramethylpiperidine-1-oxyl (TEMPO)-ferric chloride is described. Addition of sodium nitrite to the system results in the regeneration of ferric ions, making the whole system catalytic.
The invention disclosed in this application relates to an improved process for the resolution of a racemic mixture of 5-[2-[2-ethoxyphenoxy) ethylamino] propyl]-2-methoxy benzene sulfonamide (tamsulosin) employing BPA either S or R form to obtain enantiomerically hoghly pure R and S-isomer
"Enzymatic Process for the Preparation of (2S)-2-[(4R)-2-oxo-4-propyI pyrrolidine-l-yI]-butyric acid and its conversation into Brivaracetam" :
A process for the preparation of Brivaracetam, an anti-convulsion drug, is provided comprising enzymatic conversion of (2RS)-2-[ (4R)-2-oxo-4-propyl-pyrrolidin-l-yl] butyr...
A process for the preparation of Molnupiravir, an antiviral drug under investigation for the treatment of Covid-19, is provided comprising reacting 2-3-isopropylidene cytidine with isobutyric anhydride in the presence of a base to obtain 5'-isobutyric ester having an amide impurity. Treatingthe reaction mixture with...
" A Process for Preparing Brivaracetam"
A process for the preparation of Brivaracetam, an anti-convulsion drug, is provided comprising Hofmann rearrangement of (S)-3-(2-(chloroamino)-2-oxoethyl) hexanoic acid, followed by cyclization resulting in (R)-4-propyl-pyrrolidin-2-one which on condensation with bromo butyri...
"Process for the Preparation of Gabapentin"
The invention discloses a new process for the preparation of Gabapentin which comprises the reaction of spiro[cyclohexane-]59"-(3,7-diazabicyclo-[3.3.1]nonane)]-2",4",6!,8"-tetraone (diimide) with an alkali to obtain 1,1-cyclohexane diaceitic acid monoamide (CDMA). CDMA o...
The invention is related to a process for preparing 4-isopropyl cyclohexane earboxylic acid of formula (I) comprising hydrogenating cumic acid of formula (II) in presence of ruthenium catalyst in alkaline aqueous solution followed by acid treatment.
The invention disclosed in this apposition relates to an improved process for the preparation of N,N-dimethyl-3-(4-methyl-benzoyl)-propanolamine from the free acid via its halide by using N,N-dimethylammonium – N1 N1 -dimethyl carbonates, both as a solvent and reagent. The said propionamide is a key interme...
Process for the Preparation of Vilazodone Hydrochloride and Its Polymorph
A crystalline vilazodone hydrochloride has been prepared by reacting vilazodone free base with trimethylsilyl chloride using isopropanol as the solvent.
A process for the preparation of (R)-4-propyl-pyrrolidine-2-one, is provided comprising enzymatic conversion of dimethyl 3-propyl pentanedioate selectively into (S)-3-(2-methoxy-2-oxoethyl) hexanoic acid using Novozyme's Promea® enzyme, amidation of {S)-3-(2-methoxy-2-oxoethyl) hexanoic acid, followed by ester hydro...
" A Novel Process for the Preparation of Valitramiprosate "
A novel and economically viable green process for the preparation of 3-[[(2S)-2-amino-3-methyl-1-oxobutyl] amino]-1-propanesulfonic acid (Formula 1), also known as Valitramiprosate (ALZ-801), with excellent yield and high degree of both chemical and chiral...
Process for the Preparation of FMOC-GLY-THR (PSI (ME, ME) PROJ-OH The present invention describes a process for the preparation of Fmoc-Gly-Thr [Psi (Me, Me) pro]-OH by reacting Fmoc-glycyl chloride with N, O-Bis(trimethylsilyl)-threonine trimethylsilyl ester, in the presence of a base, to obtain Fmoc-Gly-(O-trime...
[Class : 42] Medical And Pharmaceutical Research, Design And Development Services; Pharmaceutical Drug Development Services For Third Parties; The Scientific Research For Medical Services