Synthesis of Difluorinated Enynes through Sonogashira-Type Coupling

Org Lett. 2016 Nov 4;18(21):5688-5691. doi: 10.1021/acs.orglett.6b02919. Epub 2016 Oct 17.

Abstract

The Sonogashira-type coupling of 2,2-difluoroethenyl tosylate with a variety of aliphatic and aromatic terminal alkynes proceeds smoothly even at room temperature to produce the corresponding difluorinated enyne derivatives. 2,2-Difluoroethenyl tosylate is a useful difluoroethenyl source because of its ready availability from 2,2,2-trifluoroethanol. Some of the obtained enynes exhibit strong fluorescence in the solid state. Further derivatization of a difluorinated enyne through Rh(III)-catalyzed oxidative coupling has also been examined.

Publication types

  • Research Support, Non-U.S. Gov't