Reaction of Thiocarbonyl Fluoride Generated from Difluorocarbene with Amines

Angew Chem Int Ed Engl. 2017 Dec 22;56(52):16669-16673. doi: 10.1002/anie.201710186. Epub 2017 Nov 30.

Abstract

The reaction of thiocarbonyl fluoride, generated from difluorocarbene, with various amines under mild conditions is described. Secondary amines, primary amines, and o-phenylenediamines are converted to thiocarbamoyl fluorides, isothiocyanates, and difluoromethylthiolated heterocycles, respectively. Thiocarbamoyl fluorides were further transformed into trifluoromethylated amines by using a one-pot process. Thiocarbonyl fluoride is generated in situ and is rapidly fully converted in one pot under mild conditions; therefore, no special safety precautions are needed.

Keywords: amines; difluorocarbene; difluoromethylthiolation; fluorine; thiocarbonyl fluoride.

Publication types

  • Research Support, Non-U.S. Gov't