CAS: 148550-51-0; Ethyl 2-(Methylsulfonyl)Pyrimidine-5-Carboxylate

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914208-17-6 73781-88-1 1368165-24-5

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ethyl 2-(methylthio)pyrimidine-5-carboxylate 4-chloro-2-methanesulfanylpyrimidine-5-carboxylic acid ethyl ester ethyl 2,4-bis(methylthio)pyrimidine-5-carboxylate2-[Acetyl-(2-ethynyl-phenyl)-amino]-pyrimidine-5-carboxylic acid ethyl ester ethyl 2-(4-(hydroxymethyl)piperidin-1-yl )pyrimidine-5-carboxylate ethyl 2-{6-[(4-fluorobenzyl)amino]-3-azabicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxylate ethyl 2-{6-[(4-chlorobenzyl)amino]-3-azabicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxylate

2-甲硫基-5-嘧啶羧酸乙酯置于间氯过氧苯甲酸体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,以0.37 G的收率获得2-甲砜基-5-嘧啶甲酸乙酯
参考文献:基于吴茱萸碱的拓扑异构酶 (Top)/组蛋白脱乙酰酶 (Hdac) 双抑制剂的设计,合成和构效关系
标题:基于吴茱萸碱的拓扑异构酶 (Top)/组蛋白脱乙酰酶 (Hdac) 双抑制剂的设计,合成和构效关系
摘要:在拓扑异构酶(top)和组蛋白去乙酰化酶(hdac)抑制剂协同作用的基础上,设计合成了一系列基于吴茱萸碱的新型top/hdac双重抑制剂.系统的构效关系 (Sar) 研究导致化合物29B和45B的发现,它们同时抑制 Top 和 Hdac,并对 Hct116 细胞系表现出有效的抗肿瘤活性.化合物29B和45B有效诱导 G2 细胞周期阻滞的细胞凋亡,并显着抑制 Hct116 细胞中的细胞 Hdac,具有非常好的体外代谢稳定性.总的来说,这项工作为基于吴茱萸碱的 Top/hdac 双抑制剂提供了有价值的 Sar 信息和先导化合物.
Doi:10.1016/j.Bioorg.2022.105702

专利信息

专利号:US-2011183958-A1
优先权日:2008-10-17
标 题 :Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：POWELL DAVID; TRANMER GEOFFREY K
权利人:MERCK FROSST CANADA LTD
摘要:Azetidine derivatives of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis.