Synthesis of Diverse Boron-Handled N-Heterocycles via Radical Borylative Cyclization of N-Allylcyanamides

Org Lett. 2018 Dec 7;20(23):7558-7562. doi: 10.1021/acs.orglett.8b03303. Epub 2018 Nov 14.

Abstract

A synthetic method based on radical borylation/cyclization cascades of N-allylcyanamides was developed to construct diverse boron-substituted N-heterocycles. In the reaction process, the N-heterocyclic carbene-boryl radical underwent a chemo- and regioselective addition to the alkene moiety, followed by cyclization with the N-cyano group. The resulting amide-iminyl radical intermediates underwent further reactions to afford various boron-tethered N-heterocyclic molecules. Further transformations to access synthetically useful building blocks were also demonstrated.

Publication types

  • Research Support, Non-U.S. Gov't