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:US-6514997-B2 优先权日:1999-12-03 标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:DRAGOVICH PETER S; PRINS THOMAS J; ZHOU RU; JOHNNSON JR THEODORE O 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: n where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-2025206703-A1 优先权日:2022-04-01 标题:Process for preparing ((1s,2s)-2-(5-methylpyridin-2-yl)cyclopropyl)methanol 发明人:ARREDONDO JUAN D; CAO YANG; CHUNG JOHN Y L; LI HONGMEI 权利人:MERCK SHARP & DOHME LLC 摘要:Described is an efficient, scalable synthesis of compounds such as ((1S,2S)-2-(5-methylpyridin-2-yl)cyclo-propyl)m ethanol, which contains a disubstituted cyclopropane with two stereogenic centers and represents a significant challenging synthetic target.