CAS: 110221-44-8; 2-((2S,6R)-6-(((S)-1-Ethoxy-1-Oxo-4-Phenylbutan-2-yl)Amino)-5-Oxo-2-(Thiophen-2-yl)-1,4-Thiazepan-4-yl)Acetic Acid Hydrochloride

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CAS号110221-37-9 (S)-ethyl 2-(((... | CAS号34312-77-1 反式-2-(2-硝基乙烯基)噻吩 | CAS号1914-59-6 (3e)-2-氧代-4-苯基丁-3-烯酸 | CAS号110143-65-2 2-oxo-4-phenylb... | CAS号102090-86-8 N-t-butoxycarbo... | CAS号110143-66-3 D-2-hydroxy-4-p... | CAS号29678-81-7 (R)-2-羟基-4-苯丁酸 | CAS号90315-82-5 (|R|)-(-)-2-羟基-... | CAS号88767-98-0 (R)-4-苯基-2-(三氟甲... | CAS号110221-53-9 替莫普利

N-T-Butoxycarbonyl-S-[2-Nitro-1-(2-Thienyl)Ethyl]-L-Cysteine置于palladium On Activated Charcoal N-甲基吗啉,盐酸,叠氮磷酸二苯酯,氢气,Sodium Hydride,溶剂黄146,三乙胺体系中,用 1,4-二氧六环,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,25.0~70.0 °C,303.98 Kpa 条件下,反应 62.0H,反应生成盐酸替莫普利
参考文献:Angiotensin-Converting Enzyme Inhibitors. Perhydro-1,4-Thiazepin-5-One Derivatives
标题:Angiotensin-Converting Enzyme Inhibitors. Perhydro-1,4-Thiazepin-5-One Derivatives
摘要:Alpha-[6-[[(S)-1-(Ethoxycarbonyl)-3-Phenylpropyl]Amino]-5-Oxoperhydro-1,4-Thiazepin-4-Yl]Acetic Acids (Monoester Monoacids) And Their Dicarboxylic Acids Having The Hydrophobic Substituents At The 2-Or 3-Position Of The Thiazepinone Ring Were Prepared And Assayed For Angiotensin-Converting Enzyme (Ace) Inhibitory Activity. The Dicarboxylic Acids Having The Pseudoequatorial Amino Groups At The 6-Position And The Pseudoequatorial Hydrophobic Substituents At The 2-Or 3-Position Of The Chair Conformation Of The Thiazepinone Ring Had Potent In Vitro Inhibitory Activity. The Monoester Monoacids Having The Hydrophobic Substituents At The 2-Position Suppressed Pressor Response To Angiotensin I For A Longer Duration Than Those Having The Substituents At The 3-Position When Administered Orally. The Structure-Activity Relationship Was Studied By Conformational Energy Calculations Of The Thiazepinone Ring.
Doi:10.1021/jm00394A009