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Asymmetric synthesis of trifluoromethyl-piperidine based gamma-amino acids and of trifluoromethyl-indolizidines

  作者 JATOI WAHID BUX; DESIRONT AGNES; JOB AURELIE; TROIN YVES; CANET JEANLOUIS  
  选自 期刊  Journal of Fluorine Chemistry;  卷期  2013年145-1;  页码  8-17  
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[摘要]The asymmetric synthesis of trifluoromethyl-piperidine-based gamma-aminoacids and of indolizidines bearing a trifluoromethyl group is reported. These rarely described compounds are prepared in a highly enantio-enriched form employing as key step an intramolecular Mannich type process, involving an enantiopure Tfm-aminoketal and ethyl oxobutenoate as aldehyde partner. Used strategy together with obtained compounds allows the access to a wide range of Tfm-N-(poly)heterocycles, structures of obvious interest for the research of new bioactive drugs. (c) 2012 Elsevier B.V. All rights reserved.

 
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