Process and intermediates for the preparation of aryl...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/74 (2006.01) C07D 401/12 (2006.01) C07D 471/04 (2006.01)

Patent

CA 1255301

425 6197-166 ABSTRACT OF THE INVENTION PROCESS AND INTERMEDIATES FOR THE PREPARATION OF ARYL SUBSTITUTED PYRIDO[1,4]BENZODIAZEPINES A process for preparing pyrido[1,4]benzodiazepines having antidepressant activity illustrated by the formula: Image 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 and wherein in the process condensation of an amino-chloropyridine with an aryl(aminophenyl)methanone 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.

478110

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