An expeditious synthesis of the MDM2-p53 inhibitor AM-8553.
J Am Chem Soc
; 134(30): 12855-60, 2012 Aug 01.
Article
in En
| MEDLINE
| ID: mdl-22734631
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.
Full text:
1
Database:
MEDLINE
Main subject:
Piperidones
/
Tumor Suppressor Protein p53
/
Proto-Oncogene Proteins c-mdm2
/
Acetates
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Year:
2012
Type:
Article