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NOVEL AND PRACTICAL SYNTHESIS OF CANDESARTAN CILEXETIL

  作者 MAO YONGJUN; XIONG RUISHENG; LIU ZHENG; LI HAIHONG; SHEN JINGKANG; SHEN JINGSHAN  
  选自 期刊  Heterocycles;  卷期  2010年81-6;  页码  1503-1508  
  关联知识点  
 

[摘要]A novel and convergent synthetic route of candesartan cilexetil (API of Atacand), an effective angiotensin II receptor blocker, is described. Cleavage of the N-Boc and N-trityl protective group are implemented simultaneously and formation of the benzimidazole ring is conducted at the last step of this route, which gives candesartan cilexetil in 55% yield over six steps with 99.1% purity (HPLC).

 
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