(2E)-4-(二甲基氨基)-2-丁烯酸甲酯置于sodium Hydroxide,水,盐酸体系中,用 甲醇,水 作为反应溶剂,化学反应 1.0H,以51%的收率获得产物反式-4-二甲基胺基巴豆酸盐酸盐 参考文献: Substituted Tricyclic Compounds And Methods Of Use Thereof[fr] Composés Tricycliques Substitués Et Leurs Procédés D'Utilisation 标题: Substituted Tricyclic Compounds And Methods Of Use Thereof[fr] Composés Tricycliques Substitués Et Leurs Procédés D'Utilisation 摘要:这项发明涉及新颖化合物及其制备方法,治疗疾病的方法,特别是癌症,包括给予这些化合物,以及制备用于治疗或预防疾病,特别是癌症的药物组合物的方法.
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:US-7126025-B2 优先权日:2003-01-21 标 题 :Synthesis of 4-(amino)-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines 发明人:CONSIDINE JOHN LEO; DAIGNEAULT SYLVAIN; CHEW WARREN; IERA SILVIO; DUNCAN SCOTT MASON; REN JIANXIN 权利人:WYETH CORP 摘要:This invention provides a compound of Formula (I): n nwhereinn S 1 and S 2 are each independently, hydrogen, alkyl, alkenyl, alkynyl, aralkyl, substituted or unsubstituted aryl, and S 1 and S 2 together with the nitrogen to which they are attached form a nitrogen containing heteroaryl and a pharmaceutically acceptable salt thereof; a method of preparing the compound of Formula (I), and use of the compound of Formula (I) in the preparation of 3-cyano quinolines.
专利号:US-2004162442-A1 优先权日:2003-01-21 标 题 :Synthesis of 4-(amino)-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines
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:CA-2514550-A1 优先权日:2003-01-21 标题:Synthesis of 4amino-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines