Collect. Czech. Chem. Commun. 1990, 55, 797-808

Potential neuroleptics of the orthopramide series; Synthesis of N-(3-(tert.amino)propyl)-5-sulfamoyl-2-methoxybenzamides

Vladimír Valenta, Marie Vlková, Jiří Holubek, Emil Svátek, Jiřina Metyšová and Miroslav Protiva

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


Heating ethyl 5-sulfamoyl-2-methoxybenzoate with a series of twelve 3-(tert.amino)propylamines (IIIa-IIIl) afforded the title compounds IIa-IIl which were transformed to salts and subjected to pharmacological screening as potential neuroleptics of the sulpiride series. Only compounds IId (hydrogen oxalate, VUFB-15 453) and IIg (methanesulfonate, VUFB-15 397) showed indications of the desired psychotropic activity.