Related Experiment Video
Updated: May 21, 2026

05:17
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
An expeditious synthesis of the MDM2-p53 inhibitor AM-8553
Brian S Lucas1, Benjamin Fisher, Lawrence R McGee
1Department of Medicinal Chemistry, Amgen, Inc., S. San Francisco, California 94080, United States. blucas@amgen.com
Journal of the American Chemical Society
|June 28, 2012
Abstract:
The development of the structurally complex MDM2/p53 inhibitor AM-8553 was impeded by the low yield of the initial synthesis. A second generation synthesis is described that features a Noyori dynamic kinetic resolution, a highly diastereoselective allylation, and a novel oxazoline-assisted piperidinone forming reaction to provide AM-8553 in 35.6% yield and 11 steps.
