Process development of GSK1120212B: a novel MEK inhibitor for the treatment of cancer

摘要

GSK1120212B is a novel MEK inhibitor in development for a variety of cancer indications. The process developed for the commercial manufacture of GSK1120212B will be presented. The process uses some novel chemistry such as amidine reduction to introduce an N-methyl group, a double acylation reaction mediated by trichloroacetic anhydride and an interesting late stage rearrangement reaction to produce the drug substance itself.