专利号:US-5068360-A 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno(3,2-C)pyridine derivatives therefrom 发明人:DEHOFF BRADLEY S 权利人:SYNTEX INC 摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:US-5191090-A 优先权日:1990-01-25 标题:Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno[3,2-c]pyridine derivatives therefrom 发明人:DEHOFF BRADLEY S 权利人:SYNTEX INC 摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:US-6608202-B1 优先权日:2001-08-21 标题:Process of synthesis of a tricyclic ketone intermediate 发明人:DORAN HENRY J; O'NEILL PAT M; WILLIAMS ROBERT P 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen,and intermediates therefor from easily available starting materials by a simple route.
专利号:US-4997945-A 优先权日:1990-01-25 标 题:Carbamate salts of 2-(2'-thienyl)alkylamines 发明人:KHATRI HIRALAL N 权利人:SYNTEX INC 摘要:The carbamate salt of 2-(2'-thienyl)-alkylamines and particularly the ethylamine and its method of synthesis are disclosed. The carbamate salt of 2-(2'-thienyl)ethylamine is a stable, easily transportable crystalline material that can be converted to 2-(2'-thienyl)ethylamine, a useful intermediate in the synthesis of 5[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine hydrochloride, also known as ticlopidine hydrochloride. The synthesis is carried out by reacting an amine of formula (I): (I) with CO2 in a hydrocarbon solvent to obtain the carbamate salt of formula II: II
专利号:US-7189864-B2 优先权日:1990-11-19 标 题:Method of preparing intermediates useful in synthesis of retroviral protease inhibitors 发明人:NG JOHN S; PRZYBYLA CLAIRE A; MUELLER RICHARD A; VAZQUEZ MICHAEL L; GETMAN DANIEL P 权利人:SEARLE & CO 摘要:A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
专利号:US-6022996-A 优先权日:1990-11-19 标 题 :Method for making intermediates useful in synthesis of retroviral protease inhibitors 发明人:NG JOHN S; PRZYBYLA CLAIRE A; MUELLER RICHARD A; VAZQUEZ MICHAEL L; GETMAN DANIEL P 权利人:SEARLE & CO 摘要:A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
[参考文献]: Christophe Duplais, Et Al. Cross-Couplings Between Benzylic And Aryl Halides "On Water": Synthesis Of Diarylmethanes. Chem Commun (Camb). 2010 Jan 28;46(4):562-4.
合成参考文献
摘要:Snaith, J. S., Science of Synthesis Knowledge Updates, (2011) 2, 173. 摘要:Pitaval, A.; Echavarren, A. M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 592. 摘要:Murata, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 466.