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(Z)-5-(4-Fluorophenyl)pent-4-enoic Acid: A Precursor for Convenient and Efficient Synthesis of the Antihypercholesterolemia Agent Ezetimibe

  作者 SOVA MATEJ; MRAVLJAK JANEZ; KOVAC ANDREJA; PECAR SLAVKO; CASAR ZDENKO; GOBEC STANISLAV  
  选自 期刊  Synthesis;  卷期  2010年-20;  页码  3433-3438  
  关联知识点  
 

[摘要]A convenient and efficient total synthesis of ezetimibe, an intestinal cholesterol absorption inhibitor and useful anticholesteremic agent, is described. Based on (Z)-5-(4-fluorophenyl)pent-4-enoic acid as a starting compound, and taking the synthesis through further Z-configured intermediates, the total yield is remarkably increased, compared with the use of the corresponding E-configured starting substances or intermediates.

 
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