专利号:WO-2011092618-A1 优先权日:2010-01-28 标题 :Method for the preparation of fluazinam 发明人:PASTORIO ANDREA; MORA CLAUDIA 权利人:FINCHIMICA SRL; PASTORIO ANDREA; MORA CLAUDIA 摘要:A method for the synthesis of 3-chloro, N- (3-chloro-5- trifluoromethyl-2-pyridyl), α, α, α-trif luoro, 2,6-dinitro- p-toluidine (Fluazinam) comprises an amination reaction of a pyridine, to obtain 2-amino, 3-chloro, 5- trif luoromethylpyridine, the addition of a strong base to the 2-amino, 3-chloro, 5-trif luoromethylpyridine, and a formation reaction of Fluazinam by coupling of the 2- amino-3-chloro-5-trif luoromethylpyridine with the 2,4- dichloro, 3,5-dinitro, benzotrif luoride. The amination reaction is conducted with anhydrous ammonia in an organic solvent. Furthermore, the coupling reaction as above takes place directly in the solution of Pyridine 2 coming from the amination step.
专利号:US-7812161-B2 优先权日:2007-03-05 标 题 :Synthesis of GlyT-1 inhibitors 发明人:PFLEGER CHRISTOPHE; WALDMEIER PIUS; WANG SHAONING 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for preparation of a compound of formula I n nwhereinn Het, R 1 , R 2 , R 3 , and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
专利号:WO-2008107334-A2 优先权日:2007-03-05 标题:Process for the synthesis of glyt-1 inhibitors
专利号:US-2008221327-A1 优先权日:2007-03-05 标题:Synthesis of glyt-1 inhibitors
专利号:EP-2131843-B1 优先权日:2007-03-05 标题 :Process for the synthesis of glyt-1 inhibitors
专利号:CN-110143916-B 优先权日:2019-05-12 标题 :Synthesis process of fluazinam
摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 654. 摘要:Li, L.; Biscoe, M. R., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 828.