N-(Aminophenyl) oxamic acids and esters as potent, orally active antiallergy agents

DH Klaubert, JH Sellstedt, CJ Guinosso…

Index: Klaubert, Dieter H.; Sellstedt, John H.; Guinosso, Charles J.; Capetola, Robert J.; Bell, Stanley C. Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 742 - 748

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Citation Number: 32

Abstract

Method M. 7-Chloro-4, 9-dihydro-4-methyl-9-oxopyrazolo [5, 1-b] quinazoline-2-carbonitrile. 7-Chloro-4, g-di-hydro-4-methyl-9-oxopyrazolo [5, 1-b] quinazoline-2-carboxamide (3 g, 0.011 mol) was heated at 56" C with thionyl chloride (1.6 mL, 0.022 mol) and DMF (35 mL) for 18 h. The resulting clear solution was evaporated to dryness, and the residue was treated with water (600 mL). After the solution was left standing for 1 h, the crude nitrile was ...