发明公开
EP3089961A1 PROCESS FOR THE MANUFACTURE OF (E)-4-N,N-DIALKYLAMINO CROTONIC ACID IN HX SALT FORM AND USE THEREOF FOR SYNTHESIS OF EGFR TYROSINE KINASE INHIBITORS
有权
用于生产（E）-4-N，N-二烷基氨基巴豆酸IN HX盐形式及其用途用于合成的EGFR酪氨酸激酶抑制剂的
- 专利标题： PROCESS FOR THE MANUFACTURE OF (E)-4-N,N-DIALKYLAMINO CROTONIC ACID IN HX SALT FORM AND USE THEREOF FOR SYNTHESIS OF EGFR TYROSINE KINASE INHIBITORS
- 专利标题（中）： 用于生产（E）-4-N，N-二烷基氨基巴豆酸IN HX盐形式及其用途用于合成的EGFR酪氨酸激酶抑制剂的
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申请号： EP14828037.3申请日： 2014-12-23
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公开(公告)号： EP3089961A1公开(公告)日： 2016-11-09
- 发明人: ZHENG, Juncheng , DENG, Da , LV, Guanghua , YAN, Jun , BRANDENBURG, Joerg , KROEBER, Jutta , SCHOLZ, Ulrich
- 申请人： Boehringer Ingelheim International GmbH
- 申请人地址： Binger Strasse 173 55216 Ingelheim am Rhein DE
- 专利权人： Boehringer Ingelheim International GmbH
- 当前专利权人： Boehringer Ingelheim International GmbH
- 当前专利权人地址： Binger Strasse 173 55216 Ingelheim am Rhein DE
- 代理机构： Simon, Elke Anna Maria
- 优先权： PCT/CN2013/091071 20131231
- 国际公布： WO2015101554 20150709
- 主分类号： C07C227/10
- IPC分类号： C07C227/10 ; C07C227/18 ; C07C229/30 ; C07D405/04
摘要：
The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein R1 and R2 independently denote C1-3-alkyl groups and X− denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.
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