Process Development of a Diacyl Glycerolacyltransferase-1 Inhibitor

Autor: Seble Wagaw, Andrew S. Judd, Jianzhang Mei, Kenneth M. Engstrom, Andrew J. Souers, Gang Zhao, Brian J. Kotecki, Philip R. Kym, Matthew M. Ravn
Rok vydání: 2010
Předmět:
Zdroj: Organic Process Research & Development. 14:417-424
ISSN: 1520-586X
1083-6160
DOI: 10.1021/op900310v
Popis: A synthesis of a selective diacyl glycerolacyltransferase-1 (DGAT-1) inhibitor, 1, is described. The synthesis illustrates a diketone Favorskii reaction on 9 in place of the more common ketoester variant for generation of the dicarboxycyclopentane core, the development of an efficient classical resolution of a key cyclopentyl ketoacid intermediate 4, and an ambient temperature Suzuki−Miyaura coupling which avoids epimerization of the labile aryl ketone of 1.
Databáze: OpenAIRE