Palladium-Catalyzed Hiyama Cross-Couplings of Arylsilanes with 3-Iodoazetidine: Synthesis of 3-Arylazetidines

J Org Chem. 2019 Oct 4;84(19):12358-12365. doi: 10.1021/acs.joc.9b01715. Epub 2019 Sep 26.

Abstract

The first palladium-catalyzed Hiyama cross-coupling reactions of arylsilanes with 3-iodoazetidine were described. The protocol provides a convenient access to a variety of useful 3-arylazetidines which are of great interest in pharmaceutical laboratories in moderate to good yields (30%-88%). In addition, this strategy has the advantage of easy operation and mild reaction conditions.

Publication types

  • Research Support, Non-U.S. Gov't