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-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-4349681-A 优先权日:1979-12-24 标题:2-Amino-3-chloro-5-trifluoromethylpyridine 发明人:YOKOMICHI ISAO; HAGA TAKAHIRO; NAGATANI KUNIAKI; NAKAJIMA TOSHIO 权利人:ISHIHARA MINING & CHEMICAL CO 摘要:A novel compound, 2-amino-trifluoromethyl-halogenopyridine, is provided, which is prepared by amination of a 2-halogeno-trifluoromethyl-halogenopyridine or by halogenation of 2-amino-trifluoromethylpyridine. This compound is useful as an intermediate for synthesis of agricultural chemicals and medicines.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-8648203-B2 优先权日:2005-11-23 标 题:Process for preparing pyridinamines and novel polymorphs thereof 发明人:COHEN SHLOMI; ZAMIR SHARONA 权利人:COHEN SHLOMI; ZAMIR SHARONA; MAKHTESHIM CHEM WORKS LTD 摘要:The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-α,α,α-trifluoro-2,6-di-nitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.