4.6 Article

Flow trifluoromethylation of carbonyl compounds by Ruppert-Prakash reagent and its application for pharmaceuticals, efavirenz and HSD-016

Journal

RSC ADVANCES
Volume 6, Issue 86, Pages 82716-82720

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c6ra19790f

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Funding

  1. Aichi Science & Technology Foundation
  2. JSPS KAKENHI [JP 16H01142]
  3. Platform Project for Supporting in Drug Discovery and Life Science Research (Platform for Drug Discovery, Informatics, and Structural Life Science) from Japan Agency for Medical Research and Development (AMED)
  4. Grants-in-Aid for Scientific Research [16H01142] Funding Source: KAKEN

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The Ruppert-Prakash reagent is the most powerful and well-documented reagent for trifluoromethylation. Despite its versatility, no general method exists for its use in a flow system. Here we report the first flow trifluoromethylation of carbonyl compounds and its utility for drug synthesis of efavirenz and HSD-016, including preliminary results of enantioselective variants.

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