Conversion of N-alkylaminobenzophenones to benzodiazepines in vivo

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Abstract
5-Chloro-2-[3-methyl-5-(dimethylamino)methyltriazol-4-yl]benzophenone can undergo N-dealkylation and ring closure in vivo to form the corresponding benzodiazepine. The in vivo conversion occurs in mice, rats and monkeys. A variety of substituted aminobenzophenone compounds were also able to undergo these conversions. The conversions to benzodiazepines were confirmed by a comparison of retention times on a gas chromatograph as well as through the use of a gas chromatographic mass spectrometer. The results did not prove that the N-alkylaminobenzophenones were devoid of activity, but suggest that their observed pharmacological activity may be due to the formation of the corresponding benzodiazepines.