2-溴-6-氰基吡啶置于盐酸,Palladium Diacetate,Caesium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 1,4-二氧六环 用作溶剂,化学反应 15.25H,反应生成2-氨基-6-氰基吡啶 参考文献:Efficient Indoles And Anilines Syntheses Employing Tert-Butyl Sulfinamide As Ammonia Surrogate 标题:Efficient Indoles And Anilines Syntheses Employing Tert-Butyl Sulfinamide As Ammonia Surrogate 摘要:Tert-Butyl Sulfinamide Is An Ammonia Equivalent For The Palladium-Catalyzed Amination Of Aryl Bromides And Aryl Chlorides. Using These Amine Derivatives,It Has Been Observed That Indoles And Anilines With Sensitive Functional Groups Can Be Readily Prepared. This Surrogate Has Also Been Used For The Synthesis Of Indoles From 2-Halophenols Using Palladium Catalyzed Cross Coupling Reaction As The Key Step. (C) 2011 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tetlet.2011.08.075
专利号:US-7405310-B2 优先权日:2001-03-05 标 题:Non-nucleoside reverse transcriptase inhibitors 发明人:LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA 权利人:MEDIVIR AB 摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
专利号:US-11731956-B2 优先权日:2018-10-22 标 题:Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
专利号:WO-2023071314-A1 优先权日:2021-10-29 标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound
专利号:US-12331058-B2 优先权日:2021-10-29 标 题:SHP2 and CDK4/6 dual-target inhibitory compound and pharmaceutical composition containing the same 发明人:WU XIAOXING; CHEN XIAOYU; LI WENQIANG; Shu Chengxia; LUO GUANGMEI; YANG KEXIN 权利人:UNIV CHINA PHARMA 摘要:The present invention belongs to the field of medicinal chemistry, and particularly relates to synthesis, a preparation method and the use of an inhibitor containing dual targets SHP2 and CDK4/6, wherein the inhibitor comprises three compounds of general formulas I-III and pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs thereof. According to the present invention, a class of brand-new SHP2 and CDK4/6 dual-target inhibitors are prepared by means of a pharmacophore fusion and reasonable drug design method, so that the problems of drug resistance, poor drug effect, etc., of the existing SHP2 inhibitor and CDK4/6 inhibitor are solved; the great significance of the present invention is providing the first SHP2 and CDK4/6 dual-target inhibitor, which provides a basis for solving the problem of drug resistance of kinase and phosphatase in the later period.
专利号:EP-4410794-A1 优先权日:2021-10-29 标题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound
专利号:CA-3236558-A1 优先权日:2021-10-29 标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound