N-(2,2-二甲基丙酰基)-3-(三氟甲基)苯胺置于氢氧化钾,正丁基锂体系中,用 乙二醇 作为反应溶剂,化学反应 12.0H,反应生成 2-甲基-3-三氟甲基苯胺 参考文献:Improved Process For The Preparation Of 2-Methyl-3-Trifluoromethylaniline: A Versatile Intermediate For Flunixin Synthesis 标题:Improved Process For The Preparation Of 2-Methyl-3-Trifluoromethylaniline: A Versatile Intermediate For Flunixin Synthesis 摘要:A Detailed New Experimental Investigation Into The Synthesis Of Flunixin Via 2-Methyl-3-Trifluoromethylaniline Is Described. The Coupling Process Between 2-Methyl-3-Trifluoromethylaniline And 2-Chloronicotinate Was Achieved Stoichiometrically And In High Yield,When Ethylene Glycol Was Used As Reaction Solvent At 160-Degrees-C. DOI:10.3987/com-94-6822
专利号:US-4209464-A 优先权日:1977-06-10 标题:Novel synthesis of 3-amino-2-methylbenzotrifluoride from N-(2-X-5-trifluoromethylphenyl)-S,S-dimethylsulfimide 发明人:STEINMAN MARTIN; WONG YEE S 权利人:SCHERING CORP 摘要:This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride, and to certain novel intermediates produced by the process. 3-Amino-2-methylbenzotrifluoride is a key intermediate useful in the preparation of valuable therapeutic agents such as, for example, 2-(2-methyl-3-trifluoromethyl)anilino nicotinic acid.
专利号:RU-94035759-A 优先权日:1991-12-20 标题 :Method of synthesis of 2-methyl-3-trifluoromethylaniline, derivatives of trifluoromethylpivalanilide and a method of their synthesis
专利号:US-5248781-A 优先权日:1992-09-21 标题 :Preparation of substituted anilino-nicotinic acid derivatives 发明人:MCKILLOP ALEXANDER 权利人:UNIV PRINCETON 摘要:Substituted anilino-nicotinic acid derivatives are readily prepared from the condensation of two intermediates, 2-alkyl-3-perfluoroalkyl-anilines and alkyl 2-chloronicotinates. The 2-alkyl-3-perfluoroalkyl-aniline intermediate can be prepared via a novel three step synthesis. 3-Perfluoroalkyl-anilines are reacted with an amine directing protecting group reagent to protect the amine. The protected amine is then alkylated, and finally, the directing group is removed to form the 2-alkyl-3-perfluoroalkyl-aniline intermediate. The 2-alkyl-3-perfluoroalkyl-aniline intermediate is condensed with the alkyl 2-chloronicotinate to form the anilino-nicotinic acid derivative.
专利号:IL-86787-A0 优先权日:1987-06-19 标题:Novel synthesis of 3-amino-2-methylbenzotrifluoride
专利号:US-4172095-A 优先权日:1977-06-10 标题 :Novel synthesis of 3-amino-2-methylbenzotrifluoride and the intermediates thereof
专利号:WO-8810247-A1 优先权日:1987-06-19 标题:Novel synthesis of 3-amino-2-methylbenzotrifluoride
参考文献:10.1055/s-0036-1591765|10.1055/s-0037-1609734 摘要:Rasheed O. Ruthenium-Catalyzed Ortho C(sp2)–H Amidation of Benzaldehydes with Organic Azides. Synlett. 2018 Feb 16;29(08):1033–6. doi: 10.1055/s-0036-1591765. 参考文献:10.1074/jbc.ra119.010201 摘要:Clausse V, Tao D, Debnath S, Fang Y, Tagad HD, Wang Y, Sun H, LeClair CA, Mazur SJ, Lane K, Shi Z, Vasalatiy O, Eells R, Baker LK, Henderson MJ, Webb MR, Shen M, Hall MD, Appella E, Appella DH, Coussens NP. Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. Journal of Biological Chemistry. 2019 Nov;294(46):17654–68. doi: 10.1074/jbc.ra119.010201. 参考文献:10.1177/2472555219873068 摘要:Lee OW, Austin S, Gamma M, Cheff DM, Lee TD, Wilson KM, Johnson J, Travers J, Braisted JC, Guha R, Klumpp-Thomas C, Shen M, Hall MD. Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. SLAS Discov. 2020 Jan;25(1):9–20.