Silver-Catalyzed Radical Arylphosphorylation of Unactivated Alkenes: Synthesis of 3-Phosphonoalkyl Indolines

J Org Chem. 2018 Apr 20;83(8):4681-4691. doi: 10.1021/acs.joc.8b00450. Epub 2018 Apr 3.

Abstract

A silver-catalyzed phosphorylation/cyclization cascade of N-allyl anilines was developed, allowing direct access to 3-phosphonoalkyl indolines, which were previously obtainable only via tedious procedures under harsh/toxic conditions. The unactivated double bond serves as the radical acceptor, whereas H-phosphonates or -phosphine oxides act as the radical precursor. This protocol features simple operation, broad substrate scope, and great exo selectivity, and a gram-scale synthesis could be readily carried out.

Publication types

  • Research Support, Non-U.S. Gov't