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Communication | Special issue | Vol 56, No. 1-2, 2002, pp.91-95
Published online, 1st January, 1970
DOI: 10.3987/COM-01-S(K)44
■ Synthesis and Biological Evaluation of Ketorolac Analogs

Francisco J. Lopez,* Mary-Frances Jett, Joseph M. Muchowski, Dov Nitzan, and Counde O'Yang

*Roche Bioscience, Neurobiology Unit, 3401 Hillview Avenue, Palo Alto, CA 94304, U.S.A.

Abstract

Ketorolac analogs were synthesized and biologically evaluated. For the preparation of the N-methylpyrrole Ro114-1907, and the furan Ro113-8905, a hydroxyethyl-assisted regioselective benzoylation gave intermediates (4) and (12), and subsequently a key copper-mediated ring closure gave entry to the required bicyclic compounds (7) and (15). Ro113-8905 and the thiophene Ro101-8244 significantly inhibited both the writhing response and edema formation in rat, but were less potent than Ketorolac.