Chiral Aziridinyl Radicals: An Application to the Synthesis of the Core Nucleus of FR-900482

Abstract

An asymmetric route to the core nucleus of the antitumor agent FR-900482 utilizes the cyclization of an aziridinyl radical into a functionalized indole nucleus. The route employs a selective Polonovski reaction and the Hootelé-Dmitrienko rearrangement to install two oxygen atoms.