CAS: 1186486-62-3; 4-Trans-(((S)-5-((3,5-Bis(Trifluoromethyl)Benzyl)(2-Methyl-2H-Tetrazol-5-yl)Amino)-7,9-Dimethyl-2,3,4,5-Tetrahydro-1H-Benzo[b]Azepin-1-yl)Methyl)Cyclohexanecarboxylic Acid

📜(1R,4R)-Methyl 4-((5-((3,5-Bis(Trifluoromethyl)Benzyl)(2-Methyl-2H-Tetrazol-5-yl)Amino)-7,9-Dimethyl-2,3,4,5-Tetrahydro-1H-Benzo[b]Azepin-1-yl)Methyl)Cyclohexanecarboxylate置于水,Sodium Hydroxide体系中,用 异丙醇 用作溶剂,化学反应 7.0H,反应生成反式-4-[[(5S)-5-[[[3,5-双(三氟甲基)苯基]甲基](2-甲基-2H-四氮唑-5-基)氨基]-2,3,4,5-四氢-7,9-二甲基-1H-1-苯并氮杂卓-1-基]甲基]环己烷羧酸,(1R,4S)-4-(((S)-5-((3,5-Bis(Trifluoromethyl)Benzyl)(2-Methyl-2H-Tetrazol-5-yl)Amino)-7,9-Dimethyl-2,3,4,5-Tetrahydro-1H-Benzo[b]Azepin-1-yl)Methyl)Cyclohexane-1-Carboxylic Acid
参考文献:Development Of A Hydrogenative Reductive Amination For The Synthesis Of Evacetrapib: Unexpected Benefits Of Water
标题:Development Of A Hydrogenative Reductive Amination For The Synthesis Of Evacetrapib: Unexpected Benefits Of Water
摘要:For The Synthesis Of Cholesteryl Ester Transfer Protein (Cetp) Inhibitor Evacetrapib,A Hydrogenative Reductive Amination Was Chosen To Join The Substituted Cyclohexyl Subunit To The Benzazepine Core. The Addition Of Water,Which Suppressed Undesired Epimerization Without Affecting The Rate Of Product Formation,Was Key To The Reaction'S Success. The Process Was Scaled To Produce More Than 1100 Kg Of Material.
Doi:10.1021/op500025V

专利信息

专利号:CN-107098946-A
优先权日:2016-02-23
标题:Synthesis and Application of CETP Inhibitors

专利号:CN-107098946-B
优先权日:2016-02-23
标 题:Synthesis and Application of CETP Inhibitors