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Download fileAn Expeditious Synthesis of the MDM2–p53 Inhibitor AM-8553
journal contribution
posted on 2016-02-20, 16:04 authored by Brian S. Lucas, Benjamin Fisher, Lawrence
R. McGee, Steven H. Olson, Julio C. Medina, Eugene CheungThe 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.