CAS: 1083158-65-9; 1-[4-N-Butyrylamino-3-Methyl-5-Aminophenyl]-3N-Methylbenzimidazole
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N-[2-methyl-4-(1-methylbenzimidazole)-2-yl-6-nitrophenyl]-butanamideN-((2-cyano-biphenyl-4'-methyl)amino-6-methyl-4-(1-methyl-1H-benzo[d]imidazol-2-yl)phenyl)butyramide 37H39N5O2C37H39N5O2合成工艺路线路线简述
📜N-[2-Methyl-4-(1-Methylbenzimidazole)-2-Yl-6-Nitrophenyl]-Butanamide置于10% Pd/c,氢气体系中,用 甲醇 用作溶剂,50.0 °C,1.0 Mpa 条件下,反应 12.0H,以90%的收率获得替米沙坦杂质34
参考文献:通过脱羧交叉偶合简便合成替米沙坦.
标题:通过脱羧交叉偶合简便合成替米沙坦.
摘要:提出了一种有效的血管紧张素ii受体拮抗剂替米沙坦的合成方法,该方法涉及邻苯二甲酸异丙酯(1)与2-(4-氯苯基)-1,3-二氧戊环(2C)作为关键步骤的脱羧交叉偶联(85%收率) .苯并咪唑部分是通过还原性胺化-缩合序列区域选择性地构建的,通过预先形成的苯并咪唑的烷基化取代了先前公开的途径.在收敛的合成中以35%的总产率获得产物,最长的序列由八个步骤组成.
Doi:10.1021/jo801937H
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主要参考文献
参考标题:Efficient And Improved Synthesis Of Telmisartan作者:A Sanjeev Kumar,Samir Ghosh,G N Mehta
摘要:An Efficient Synthesis Of The Angiotensin Ii Receptor Antagonist Telmisartan (1) Is Presented Involving A Cross Coupling Of 4-Formylphenylboronic Acid 10 With 2-(2-Bromophenyl)-4,4-Dimethyl-2-Oxazoline (11) As The Key Step (90% Yield). The Benzimidazole Moiety 15 Was Constructed Regioselectively Via A Reductive Amination-Condensation Sequence, Replacing The Alkylation Of The Preformed Benzimidazole Step In The Previously Published Route. This Methodology Overcomes Many Of Drawbacks Associated With Previously Reported Syntheses.
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