Direct (het)arylation of tetrahydroisoquinolines via a metal and oxidant free C(sp3)-H functionalization enabled three component reaction

Org Biomol Chem. 2019 Feb 13;17(7):1800-1804. doi: 10.1039/c8ob02309c.

Abstract

An unprecedented method for the direct arylation and heteroarylation of tetrahydroisoquinolines under metal and oxidant free conditions is reported. The arylation reactions occurred via a C(sp3)-H functionalization enabled three component condensation of tetrahydroisoquinolines, 9-fluorenone imine, and arenes without involving a pre-functionalization/pre-derivatization step. A wide range of arenes and heteroarenes participated in the reaction to provide structurally diverse arylated tetrahydroisoquinolines with good to excellent yields.

Publication types

  • Research Support, Non-U.S. Gov't