A facile synthesis of an oxidation product of terfenadine

SH Kawai, RJ Hambalek, G Just

Index: Kawai, Stephen H.; Hambalek, Robert J.; Just, George Journal of Organic Chemistry, 1994 , vol. 59, # 9 p. 2620 - 2622

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Citation Number: 47

Abstract

Terfenadine (1 I), a selective HI-histamine receptor antagonist? is a widely used antihistamine3 which is devoid of CNS effe~ ta.~ The compound is almost completely biotransformed by hepatic cytochrome P4503 to the pharmacologically active acid metabolite lo3 and the inactive metabolite azacyclonol (a, a-diphenyl-4-piperidinemethanol) in the first pas~.~ 9~ Recently, there have been reports which suggest that terfenadine is ...