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Stereoselective Synthesis of 12,13-Cyclopropyl-Epothilone B and Side-Chain-Modified Variants

  作者 SCHIESS RAPHAEL; GERTSCH JUERG; SCHWEIZER W BERND; ALTMANN KARLHEINZ  
  选自 期刊  Organic Letters;  卷期  2011年13-6;  页码  1436-1439  
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[摘要]A general strategy has been devised for the stereoselective synthesis of 12,13-cyclopropyl-epothilone B and side-chain-modified variants thereof, which relies on late stage introduction of the heterocycle through Wittig olefination of ketone 14. Formation of the macrocycle was achieved through RCM-based ring closure and introduction of the cyclopropane moiety involved a highly selective Charette cyclopropanation of allylic alcohol 7.

 
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