PROCESS FOR THE PREPARATION OF SODIUM SALT OF 1-(((1(R)-(3-(2-(7-CHLORO-2-QUINOLINYL)-ETHENYL)PHENYL)-3-(2-(1-HYDROXY-1-METHYLETHYL)PHENYL)PROPYL)SULFANYL)METHYL)CYCLOPROPANEACETIC ACID

摘要

A novel process for the preparation of a sodium salt of 1-(((1(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(1-hydroxy-1-methyl-ethyl)phenyl)propyl)sulfanyl)methyl)cyclopropaneacetic acid, comprising: a) reacting a compound of Formula 1 with methanesulfonyl chloride in the presence of a tertiary amine to yield a crude solution of a compound of Formula 2; b) filtering the crude solution of compound of Formula 2 obtained in a) to remove solid amine hydrochloride, reacting the filtrate without isolation or further purification with a compound of Formula 3, and isolating 1-(((1(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)sulfanyl)methyl)cyclopropaneacetic acid; c) reacting the 1-(((1(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)sulfanyl)methyl)cyclopropaneacetic acid isolated in b) with tert-butylamine to yield a compound of formula 4; d) isolating and purifying the compound of formula 4; and e) converting the compound of formula 4 to a compound of formula 5.