Development of practical synthesis of halichondrins

Abstract

Halichondrin B is a polyether macrolide that exhibits an extraordinary cytotoxicity in vitro and antitumor efficacy in vivo. A structurally simplified macrolactone right half segment of harichondrin B was identified to retain the potent cell growth inhibitory activity of the natural product in vitro. Kishi and coworkers developed a practical, an efficient and scalable synthesis of the right half segment of harichondrin B.