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 |
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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 |
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