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-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-4906756-A 优先权日:1988-05-10 标 题 :2-(2-nitrovinyl)thiophene reduction and synthesis of thieno[3,2-c]pyridine derivatives 发明人:LODEWIJK ERIC; KHATRI HIRALAL N 权利人:SYNTEX INC 摘要:An improved process for the reduction of 2-(2-nitrovinyl)thiophene to form 2-(2-thienyl)ethylamine employs a boron-containing reducing agent, preferably diborane. The 2-(2-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:EP-0522956-B1 优先权日:1991-07-08 标 题 :Preparation of 2-(2-thienyl) ethylamine and synthesis of thieno [3,2-C] pyridine derivatives therefrom 发明人:HARRINGTON PETER J; SANCHEZ IGNACIO H 权利人:SANOFI SA 摘要:Compounds of the formulae: and wherein: R<1>, R<2>, R<3> and R<4> are independently hydrogen, lower alkyl of one to six carbon atoms, aryl or substituted aryl; are advantageously converted to isocyanurate compounds, 2-(2-thienyl)ethylamine compounds and thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
专利号:US-8906915-B2 优先权日:2009-12-17 标 题:Compounds, compositions, and methods for controlling biofilms 发明人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S 权利人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S; UNIV LEUVEN KATH 摘要:The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 268. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 239. 摘要:Chanda, A.; Fokin, V. V., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 734.