4-(三氟甲基)-1H-咪唑置于ammonium Hydroxide体系中,化学反应 8.0H,以87%的收率获得产物1H-咪唑-4-甲腈 参考文献:A Convenient Procedure For The Preparation Of 4(5)-Cyanoimidazoles 标题:A Convenient Procedure For The Preparation Of 4(5)-Cyanoimidazoles 摘要: DOI:10.1021/jo00366A037
专利号:US-9303046-B2 优先权日:2012-08-07 标 题:Process for the preparation of heterocyclic ester derivatives 发明人:BONGARTZ JEAN-PIERRE ANDRÉ MARC; STAPPERS ALFRED ELISABETH; TELEHA CHRISTOPHER A; WEERTS KOEN JOHAN HERMAN; WILSON KENNETH J 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to a process for the preparation of heterocyclic ester derivatives of formula I n nwherein A 1 , SEM, and W 1 are as defined herein. Such compounds are useful as intermediates in the synthesis of derivatives useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.
专利号:WO-2010149360-A1 优先权日:2009-06-26 标题:Process for the preparation of benzimidazoles 发明人:HANSELMANN PAUL; WONG HEILAM; KLEGRAF ELLEN; ZARAGOZA DOERWALD FLORENCIO; DING ZUNLIANG; LONG JUN 权利人:LONZA AG; HANSELMANN PAUL; WONG HEILAM; KLEGRAF ELLEN; ZARAGOZA DOERWALD FLORENCIO; DING ZUNLIANG; LONG JUN 摘要:Substituted benzimidazoles of formula (I), wherein R 1 and R 2 independently are hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl and R 3 is cyano or carboxy, are prepared in a multistep synthesis starting from Î? -acyl-4-halo- anilines of formula (II), wherein R 1 and R 2 are as defined above and X is chlorine or bromine.
专利号:US-2013273461-A1 优先权日:2012-04-11 标题 :Synthesis of electrocatalysts using metal-organic framework materials
专利号:US-11718586-B2 优先权日:2019-11-08 标 题:Method for preparing dexmedetomidine 发明人:DIKER KHALID; GORINS GILLES; OZANNE-BEAUDENON AURÉLIE; GOLDSTEIN CORINNE 权利人:NORCHIM 摘要:The present invention relates to a method for preparing dexmedetomidine having the following formula (I): or a pharmaceutically acceptable salt and/or solvate thereof, comprising the following successive steps: a) asymmetric hydrogenation of a methylene derivative of the following formula (II): in order to obtain dexmedetomidine, and b) optionally salifying and/or solvating dexmedetomidine in order to obtain a pharmaceutically acceptable salt and/or solvate of dexmedetomidine, wherein the methylene derivative of formula (II) is prepared from a halide of the following formula (V), in which Hal 2 represents a halogen atom such as Br, and a cyanoimidazole of the following formula (VI). The present invention relates also to methods for preparing synthesis intermediates of dexmedetomidine from the halide of formula (V) and the cyanoimidazole of formula (VI), these synthesis intermediates being the methylene derivative of formula (II), an alcohol of the following formula (III), and a ketone of the following formula (IV).
专利号:CN-106061963-B 优先权日:2013-12-20 标题 :Heterocyclic modulators of lipid synthesis and combinations thereof
专利号:CN-116987036-A 优先权日:2023-08-04 标题:A kind of synthesis method of base-promoted 4-cyanoimidazole derivatives
参考文献:10.1126/sciadv.abf8711 摘要:Schuller M, Correy GJ, Gahbauer S, Fearon D, Wu T, Díaz RE, Young ID, Carvalho Martins L, Smith DH, Schulze-Gahmen U, Owens TW, Deshpande I, Merz GE, Thwin AC, Biel JT, Peters JK, Moritz M, Herrera N, Kratochvil HT; QCRG Structural Biology Consortium, Aimon A, Bennett JM, Brandao Neto J, Cohen AE, Dias A, Douangamath A, Dunnett L, Fedorov O, Ferla MP, Fuchs MR, Gorrie-Stone TJ, Holton JM, Johnson MG, Krojer T, Meigs G, Powell AJ, Rack JGM, Rangel VL, Russi S, Skyner RE, Smith CA, Soares AS, Wierman JL, Zhu K, O'Brien P, Jura N, Ashworth A, Irwin JJ, Thompson MC, Gestwicki JE, von Delft F, Shoichet BK, Fraser JS, Ahel I. Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking. Sci Adv. 2021 Apr;7(16). 摘要:Subramanian, L. R., Science of Synthesis, (2004) 19, 100.