One-Pot Benzo[b]phosphole Synthesis through Sequential Alkyne Arylmagnesiation, Electrophilic Trapping, and Intramolecular Phospha-Friedel-Crafts Cyclization

Org Lett. 2015 Nov 20;17(22):5666-9. doi: 10.1021/acs.orglett.5b02950. Epub 2015 Nov 12.

Abstract

A one-pot multicomponent synthesis of a benzo[b]phosphole derivative has been achieved by a sequence of transition-metal-catalyzed arylmagnesiation of an internal alkyne, electrophilic trapping of the resulting alkenylmagnesium species with a dichloroorganophosphine, and an intramolecular phospha-Friedel-Crafts reaction. With appropriate arylmagnesiation and P-C bond formation conditions, the present method allows for the modular and expedient preparation of benzophospholes bearing a variety of substituents on the phosphorus atom, the C2 and C3 atoms, and the "benzo" moiety.

Publication types

  • Research Support, Non-U.S. Gov't