Fast construction of isoquinolin-1(2H)-ones by direct intramolecular C-H/N-H functionalization under metal-free conditions

Org Biomol Chem. 2020 Jan 2;18(2):225-229. doi: 10.1039/c9ob02430a.

Abstract

The general protocol for the synthesis of isoxazolidine-fused isoquinolin-1(2H)-ones was established with the help of bench stable hypervalent iodine reagent PIDA. Polycyclic six-, seven- and eight-membered N-heterocycles can be rapidly synthesized from available amides under metal-free conditions within 1 min at room temperature through C-H/N-H functionalization. Moreover, the protocol has the merits of broad substrate scope, atom economy and operational simplicity.

Publication types

  • Research Support, Non-U.S. Gov't