2-(Alkylamino) nicotinic acid and analogs. Potent angiotensin II antagonists

…, TM Zydowsky, RJ Altenbach, FZ Basha…

Index: Winn, Martin; De, Biswanath; Zydowsky, Thomas M.; Altenbach, Robert J.; Basha, Fatima Z.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 18 p. 2676 - 2688

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Citation Number: 27

Abstract

-60, X= CNHSOZC~ H~ termination by X-ray) and subsequent desulfurization of 35 with Raney nickel to give 29 (R= 5-F). The other substituents (Cl, I, NO2) at the 5-position of the nicotinic acid were introduced by way of electrophilic substitution on 36 (see scheme VI). The 5-phenyl analog was conveniently made by a palladium-catalyzed coupling reaction of the 5-iOdO ester 31 with phenyl boronic acid. The 6-hydroxy compound was prepared ...