4.5 Article

Recent Advances in Difluoromethylation Reaction

Journal

CURRENT ORGANIC CHEMISTRY
Volume 19, Issue 16, Pages 1638-1650

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1385272819666150615235605

Keywords

Direct difluoromethylation; stepwise difluoromethylation; difluoromethyl synthons; fluorinating reagent; difluorocarbene

Funding

  1. National Basic Research Program of China [2012CB821600]
  2. National Natural Science Foundation of China [21032006, 21302207, 21421002]

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Impressive progress has been achieved during the past decade in the incorporation of various fluroine-containing groups, especially lightly fluorinated groups, into organic compounds. Among them, the introduction of difluoromethyl group into a compound commonly brings about many special and important effects. Two major strategies have been developed: (1) direct transfer of a CF2H group into target molecules (direct difluoromethylation); (2) the introduction of a functionlized moiety into organic substrates followed by subsequent transformation of the functional group into hydrogen or fluorine atoms (stepwise difluoromethylation). This mini review summarizes the recent developments in the selective direct and stepwise difluoromethyaltion methods during the past six years.

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