Radical Borylative Cyclization of 1,6-Dienes: Synthesis of Boron-Substituted Six-Membered Heterocycles and Carbocycles

Org Lett. 2018 Apr 20;20(8):2360-2364. doi: 10.1021/acs.orglett.8b00694. Epub 2018 Apr 6.

Abstract

A radical borylative cyclization reaction of 1,6-dienes was developed to assemble boron-handled six-membered heterocycles and carbocycles. This reaction was initiated by the chemo- and regio-controlled addition of an N-heterocyclic carbene-boryl radical to one of the alkene tethers, followed by an intramolecular 6- exo cyclization to afford a six-membered ring framework. The utility of this method was demonstrated in the synthesis of diverse paroxetine analogues through late-stage derivatization of the boryl functional unit.

Publication types

  • Research Support, Non-U.S. Gov't