Highly enantioselective synthesis of angelmarin

摘要

Angelmarin (1), a novel anti-cancer agent, was efficiently synthesized through a highly enantioselective epoxidation and a copper cyanide-mediated esterification of the hindered alcohol as the key steps in 53% overall yield. During the course of a unique screening program using the anti-austerity strategy, Kadota, Esumi, and co-workers identified a new coumarin natural product, angelmarin (1), from an extract of Angelica pubescens, which preferentially displays strong activity against PANC-1 cancer cells under a nutrient starvation environment (Fig. 1).