An efficient multikilogram synthesis of ABT-963: A selective COX-2 inhibitor

FAJ Kerdesky, MR Leanna, J Zhang, W Li…

Index: Kerdesky, Francis A. J.; Leanna, M. Robert; Zhang, Ji; Li, Wenke; Lallaman, John E.; Ji, Jianguo; Morton, Howard E. Organic Process Research and Development, 2006 , vol. 10, # 3 p. 512 - 517

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Citation Number: 30

Abstract

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.