Process for the production of 2,6-diaminobenzonitrile derivatives
2,6-Diaminobenzonitriles, useful in the production of N-(2-cyano-3-substituted or unsubstituted amino-phenyl)oxamate and N-(2-cyano-3-substituted or unsubstituted amino-phenyl)tetrazole-5-carboxamide antiallergy and antisecretory agents, are prepared by sequential displacement of the fluoro substituents from 2,6-difluorobenzonitrile with the appropriately substituted amine.
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(2008/06/13)
N-(Aminophenyl)oxamic Acids and Esters as Potent, Orally Active Antiallergy Agents
A series of N-(2-cyano-substituted-phenyl)oxamates was prepared by acylation of the appropriate anthranilonitrile with ethyloxalyl chloride.Hydrolysis with sodium hydroxide gave the corresponding oxamic acid sodium salts.These compounds were extremely potent when tested in the rat passive cutaneous anaphylaxis (PCA assay either by the ip or the po route of administration).One of the sodium salts, oxoacetic acid sodium salt (11a, Wy-41 195), has ED50 value of 0.07 mg/kg po and has been selected for further evaluation.
Klaubert, Dieter H.,Sellstedt, John H.,Guinosso, Charles J.,Capetola, Robert J.,Bell, Stanley C.
p. 742 - 748
(2007/10/02)
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