专利号:US-9242965-B2 优先权日:2013-12-31 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 发明人:ZHENG JUNCHENG; DENG DA; LV GUANGHUA; YAN JUN; BRANDENBURG JOERG; KROEBER JUTTA; SCHOLZ ULRICH 权利人:BOEHRINGER INGELHEIM INT 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 n nwherein R 1 and R 2 independently denote C 1-3 -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.
专利号:EP-3089961-B1 优先权日:2013-12-31 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
专利号:EP-3089961-A1 优先权日:2013-12-31 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
专利号:US-2015183764-A1 优先权日:2013-12-31 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
专利号:WO-2015101554-A1 优先权日:2013-12-31 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
专利号:US-8188274-B2 优先权日:2006-01-26 标题 :Process for preparing aminocrotonylamino-substituted quinazoline derivatives 发明人:SCHROEDER JUERGEN; DZIEWAS GEORG; FACHINGER THOMAS; JAEGER BURKHARD; REICHEL CARTSEN; RENNER SVENJA 权利人:SCHROEDER JUERGEN; DZIEWAS GEORG; FACHINGER THOMAS; JAEGER BURKHARD; REICHEL CARTSEN; RENNER SVENJA; BOEHRINGER INGELHEIM INT 摘要:The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) n nwherein the groups R a , R b , R c and R d have the meanings given in the claims, as well as sulphonyl derivatives of formulan n nand the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.