专利号:EP-0439404-B1 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl) alkylamines and derivatives thereof and synthesis of 4,5,6,7- thieno [3,2-c] pyridine derivatives therefrom 发明人:KHATRI HIRALAL N; DEHOFF BRADLEY S 权利人:SANOFI SA 摘要:An improved process for the synthesis of 2-(2 min -thienyl)ethylamine from suitably functionalized derivatives of 2-(2 min -thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2 min -thienyl)ethylamine produced by this process is advantageously converted to the carbamic acid salt, which is suitably reconverted to 2-(2 min -thienyl)ethylamine, a useful intermediate in the synthesis of ticlopidine.
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-8071782-B2 优先权日:2007-10-02 标 题 :Synthesis of 1,3,4-trisubstituted and 1,3,4,5-tetrasubstituted pyrazoles 发明人:DENG XIAOHU; MANI NEELAKANDHA S 权利人:DENG XIAOHU; MANI NEELAKANDHA S; JANSSEN PHARMACEUTICA NV 摘要:This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.
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:US-5516910-A 优先权日:1991-01-31 标题:N--2--chlorobenzyl--2--oxo and n--2--chlorobenzyl--2,2--dioxo--1,2,3--oxathiazolidine derivatives, their preparation and synthesis of thieno[3,2--c]pyridine derivatives therefrom 发明人:COOPER GARY F; MCCARTHY KEITH E 权利人:SYNTEX INC 摘要:Compounds of the formula: ##STR1## wherein: A is oxo or dioxo; n R 1 , R 2 and R 3 are independently hydrogen or lower alkyl of one to six carbon atoms; n R 4 , R 5 , R 6 and R 7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo; n are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
参考文献:10.1007/s007060170057 摘要:Bogdanowicz-Szwed K, Budzowski A. Efficient Synthesis of Functionalized 2H-Thiopyrans via Hetero-Diels-Alder Reactions of an Enaminothione with Electrophilic Olefins. Monatshefte für Chemie - Chemical Monthly. 2001 Aug;132(8):947–57. doi: 10.1007/s007060170057. 参考文献:10.1007/s10562-015-1653-x 摘要:Hemmaragala NM, Abrahamse H, George BPA, Gannimani R, Govender P. Functionalized Silver Nanoparticle Catalyzed [3+2] Cycloaddition Reaction: Greener Route to Substituted-1,2,3-triazolines. Catalysis Letters. 2015 Nov 20;146(2):464–73. doi: 10.1007/s10562-015-1653-x. 参考文献:10.1007/bf00471194 摘要:Sitkin AI, Klimenko VI. Reaction of nitrogen tetroxide with 2-vinylthiophene and substituted 2-vinylthiophenes. Chemistry of Heterocyclic Compounds. 1979 Jan;15(1):34–6. doi: 10.1007/bf00471194.