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1. (WO2014190804) METHOD FOR PREPARING CRYSTAL FORM F OF ERLOTINIB HCL

Pub. No.:    WO/2014/190804    International Application No.:    PCT/CN2014/075094
Publication Date: Fri Dec 05 00:59:59 CET 2014 International Filing Date: Fri Apr 11 01:59:59 CEST 2014
IPC: C07D 239/94
Applicants: ESTEVE HUAYI PHARMACEUTICAL CO. LTD.
埃斯特维华义制药有限公司
Inventors: WINTER, Stephen
温特S.
SHANG, Yongyan
商永严
TALAVERA ESCASANY, Pedro
塔拉韦拉埃斯卡萨尼P.
BERENGUER MAIMO, Ramon
贝伦古尔马尔莫R.
ZHENG, Guorong
郑国荣
Title: METHOD FOR PREPARING CRYSTAL FORM F OF ERLOTINIB HCL
Abstract:
The present invention relates to a new method for preparing crystal form F of erlotinib HCl. The method comprises adding an erlotinib free alkali in a C4 alcohol into hydrogen chloride dissolved in an organic solvent, and crystallizing the resulting erlotinib HCl. The method of the invention has the advantages of being suitable for large-scale preparation and having reproducibility. Furthermore, the method of the present invention also comprises the conversion of the crystal form F of erlotinib HCl into other crystal forms.