169954-93-2

Upstream product

• 142569-70-8 (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methylethyl)phenyl]-propan-1-ol 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 577953-88-9 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt 
• 142522-28-9 cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate 
• 158966-92-8 montelukast 
• 151767-02-1 Montelukast sodium 
• 855473-51-7 1-(((1(R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid methyl ester 
• 169954-94-3 dicyclohexylamine 1-(((1-(R)-(3-(2-(7-chloro-2-quinolidyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methyl-ethyl)phenyl)propyl)thio)methyl)cyclopropanyl acetate 

Relevant academic research and scientific papers

AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM

The present invention disclosed herein is a cost effective, in-situ process for the preparation of montelukast or its pharmaceutically acceptable salts of formula (1) by reacting optically pure (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methyl ethyl) phenyl]-propan-I-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by insitu condensing the same with disodium salt of mercapto-cyclopropyl acetic acid of formula (3) to afford montelukast free acid in good yield and purity, then converting the montelukast free acid into its substituted amine salt of formula (4). Further the montelukast substituted amine is converted into its pharmaceutically acceptable salt.

METHOD FOR PREPARATION OF MONTELUKAST ACID IN IONIC LIQUID MEDIUM

The present invention relates to a method for preparing Montelukast acid or its sodium salt by reacting a thiol compound with a Montelukast intermediate in the presence of a base in a medium comprising an ionic liquid compound. In accordance with the inventive method, highly pure Montelukast acid or its sodium salt, which is advantageously used as a raw material in the preparation of Montelukast, a leukotriene antagonist, can be easily prepared in a high yield.

METHOD FOR PREPARING MONTELUKAST SODIUM SALTS

Disclosed is a method for preparing a montelukast sodium salt of Formula 1. The method includes coupling a methanesulfonyl compound of Formula 2 below with a compound of Formula 3 below in the presence of a bistrimethylsilylamide alkali metal salt, further adding an alkali metal base thereto and hydrolyzing the mixture by heating to prepare a compound of Formula 4 below, reacting the compound of Formula 4 with 4-tert-butylcyclohexylamine, followed by purification, to prepare an amine salt of Formula 5, and converting the amine salt of Formula 5 into a sodium salt.

METHOD FOR THE PREPARATION OF MONTELUKAST ACID IN IONIC LIQUID MEDIUM

The present invention relates to a method for preparing Montelukast acid or its sodium salt by reacting a thiol compound with a Montelukast intermediate in the presence of a base in a medium comprising an ionic liquid compound. In accordance with the inve

PREPARATION OF MONTELUKAST AND ITS SALTS

Processes for preparing montelukast acid and its salts.

MONTELUKAST BENZHYDRYL PIPERAZINE SALTS AND PROCESS FOR PREPARATION THEREOF

The invention relates to Benzhydryl piperazine salts of [R-(E)] -1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl]-3-[2-(1 -hydroxy-1-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid represented by the formula (III). Furthermore, the invention relates to the use of Benzhydryl piperazine salts of [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid represented by the formula (III) for the preparation of substantially pure [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl] -3 -[2-(1-hydroxy-1- methylethyl) phenyl] propyl] thio] methyl] cyclopropane acetic acid or its alkali, salts and pharmaceutical composition comprising the same.

PROCESS FOR THE PURIFICATION OF OPTICALLY IMPURE 2-(2-(3(S)-(3-(7-CHLORO-2-QUINOLINYL)ETHENYL)PHENYL)-3-HYDROXY-PROPYL)PHENYL-2-PROPANOL

A process for purifying an optically impure 2-(2-(3(S)-(3-(7-chloro-2-quinolinyl)- ethenyl)-phenyl)-3-(hydroxylpropyl)phenyl)-2 propanol is disclosed. The purified compound typically has an enantiomeric excess higher than 99%, and can be used to prepare montelukast and salts thereof.

PROCESS FOR THE PREPARATION OF SODIUM SALT OF L-(((L(R)-(3-(2-(7-CHLORO-2- QUINOLINYL)-ETHENYL)PHENYL)-3-(2-(L-HYDROXY-L- METHYLETHYL)PHENYL)PROPYL)SULFANYL)METHYL)CYCLOPROPANEACETIC ACID

The invention relates to a novel process for the preparation of Sodium salt of 1- (((l(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(l-hydroxy-l- methylethyl)phenyl) propyl)sulfanyl)methyl)cyclopropaneacetic acid wherein the crystalline forms of methanesulfonate and Montelukast are not isolated. Furthermore, the invention relates to a novel process for preparing salt of 1-(((1(R)- (3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(l-hydroxy-l- methylethyl)phenyl)propyl)sulfanyl)methyl)cyclopropaneacetic acid with tert- butylamine and the method for its purification to achieve pharmaceutical purity.