KOVÁNYINÉ LAX GYÖRGYI,SIMIG GYULA,BARTHA FERENC LÓRÁNT,KRASZNAI GYÖRGY,RUZSICS GYÖRGY,NAGY KÁLMÁN,MOROVJÁN GYÖRGY,BARKÓCZY JÓZSEF,KESZTHELYI ADRIENN,IMRE JÁNOS,BAGYINSZKI GÁBOR,SIPOS ÉVA,VOLK BALÁZS
申请号：
NZ61076511
公开号：
NZ610765A
申请日:
2011.11.29
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
The disclosure relates to a method for the preparation of rosuvastatin tert-tertbutylammonium (TBA) salt of the formula (III) which is an intermediate useful in the manufacture of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid, wherein the method comprises reacting a rosuvastatin ester of the formula (II) having solid crystalline form where in the formula (II) R represents methyl, ethyl or tert-butyl using a polar solvent, with 1.5 to 5 molar equivalents, of tert-butylamine in aqueous solution at a temperature between 10 °C and the boiling point of the solvent. Polymorphs of said intermediate, methods for preparation thereof and use thereof are also disclosed.
