GORE VINAYAK GOVIND,TRIPATHI ANILKUMAR,JADHAV MADHAV
申请号：
NZ60604211
公开号：
NZ606042A
申请日:
2011.07.22
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
Disclosed is a process for the preparation of a salt of erlotinib (particularly the hydrochloride salt), comprising reacting 4-chloro-6,7-bis-(2-methoxyethoxy)quinazoline and 3-ethynylaniline in methanol, wherein the reaction mixture does not contain an external acid or base. Also disclosed is a process for the preparation of erlotinib base, comprising reacting a salt of erlotinib (such as the hydrochloride salt) with a base in a solvent consisting of: (a) methanol and/or ethanol and (b) optionally water. Also disclosed is a process which comprises isolating erlotinib hydrochloride as its form A polymorph, wherein the form A polymorph exhibits an X-ray powder diffraction (XRPD) pattern comprising at least the characteristic peaks 5.6, 9.8, 18.9, 22.7 and 23.5 ±0.2 degrees 2theta.
