An Efficient Multikilogram Synthesis of ABT-963: A Selective COX-2 Inhibitor

Autor:	John E. Lallaman, Jianguo Ji, Wenke Li, Howard E. Morton, Ji Zhang, Francis A. J. Kerdesky, M. Robert Leanna
Rok vydání:	2006
Předmět:	Suzuki reaction Chemistry Organic Chemistry COX-2 inhibitor Physical and Theoretical Chemistry Combinatorial chemistry Alkoxylation
Zdroj:	Organic Process Research & Development. 10:512-517
ISSN:	1520-586X 1083-6160
Popis:	An efficient chemical process for the multikilogram synthesis of ABT-963 (3) is described. The potent and selective COX-2 inhibitor was prepared in four steps in 36% overall isolated yield from commercially available 3,4-difluoroaniline (4). The chemistry, which required no chromatography, involved a facile one-pot synthesis of the pyridazinone core, a selective alkoxylation, a high yielding Suzuki coupling, and a very efficient oxidation.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::337a8c24dfdafd064fcba98fe007c78e https://doi.org/10.1021/op060016v Zobrazit plný text záznamu