Synthesis of STM2457, a selective small-molecule inhibitor of METTL3

Abstract

STM2457, a potent and selective inhibitor of m6A methyltransferase METTL3, is a first-in-class drug candidate for cancer therapy. Herein, we present a chromatography-free synthesis of STM2457 in nine steps and 32% overall yield. In comparison to the reported route, the current approach features inexpensive raw materials, gentle reagents and simple experimental manipulations. We expect the present work supports the production of STM2457 and facilitates its therapeutic applications.