Jae Uk Jeong; Philip A. Harris; James Kang; Lara Leister; Yunfeng Lan; Joseph Romano; Xiaoyang Dong; Robert W. Marquis
Tetrahedron Lett., 2017, 58, 23, 2306-2308
https://doi.org/10.1016/j.tetlet.2017.05.001

Abstract

Two new synthetic routes were developed to prepare the RIP1 kinase inhibitor clinical candidate GSK2982772 involving a key (S)-3-amino-benzo[b][1,4]oxazepin-4-one intermediate prepared via Mitsunobu and SNAr cyclization reactions. Both routes are practical and cost effective compared to the initial medicinal chemistry route and are also applicable to kilogram scale-up to support on-going clinical studies.