ARYL SUBSTITUTED PYRIDO (1,4) BENZODIAZEPINES (PROCESS AND INTERMEDIATES)

A process for preparing pyrido[1,4]benzodiazepines having antidepressant activity illustrated by the formula:wherein Ar is pyridinyl, thienyl or phenyl; R is alkali-metal ion, hydrogen, loweralkyl or an amine or an amine precursor on the end of a hydrocarbon chain involves the condensation of an ami...

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Sprache:eng
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Zusammenfassung:A process for preparing pyrido[1,4]benzodiazepines having antidepressant activity illustrated by the formula:wherein Ar is pyridinyl, thienyl or phenyl; R is alkali-metal ion, hydrogen, loweralkyl or an amine or an amine precursor on the end of a hydrocarbon chain involves the condensation of an amino-chloro-pyridine with an aryl(aminophenyl)-methanone, which is accomplished with a strong non-nucleophilic base in stirrable admixture with an inert liquid carrier. Alternatively, condensation is accomplished sequentially using titanium tetrachloride first followed by non-nucleophilic base.