Title:
AZD9291 INTERMEDIATE AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2016/202125
Kind Code:
A1
Abstract:
Disclosed are an intermediate, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine]phenyl-2-propenamide (II), applicable in preparing AZD9291 (I) and a preparation method for the intermediate. Preparation steps comprise: 2-fluoro-4-methoxyaniline, serving as a starting material, undergoes amidation, substitution, nitrification, reduction, and guanidination reactions to produce N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine]phenyl-2-propenamide (II). Also disclosed is a method for preparing AZD9291 (I) by means of a cyclization reaction between the compound of formula II and (2E)-3- dimethylamino-1-(1-methyl-1H-indol-3-yl)-2-propen-1-one (III). The preparation method has readily available raw materials and a simple process and is economical, environmentally friendly, and suitable for industrialized production.
Inventors:
XU XUENONG (CN)
Application Number:
PCT/CN2016/081941
Publication Date:
December 22, 2016
Filing Date:
May 13, 2016
Export Citation:
Assignee:
SUZHOU MIRACPHARMA TECH CO LTD (CN)
International Classes:
C07C279/18; C07C277/08; C07C403/04
Domestic Patent References:
| WO2013014448A1 | 2013-01-31 |
Foreign References:
| CN104910049A | 2015-09-16 | |||
| US20010056123A1 | 2001-12-27 |
Attorney, Agent or Firm:
SUZHOU WISTONG INTELLECTUAL PROPERTY AGENCY (COMMON PARTNERSHIP) (CN)
苏州慧通知识产权代理事务所（普通合伙） (CN)
苏州慧通知识产权代理事务所（普通合伙） (CN)
Download PDF: