99593-25-6

The synthesis of (5-acylaminomethyl-3-carbamoyl-1H-1,2,4-triazol-1-yl)benzophenone derivatives is described. Acylation of the key intermediate, 1-benzoylphenylazo-1-aminoacetamide followed by cyclization in the presence of acid afforded 1H-1,2,4-triazole derivates. These compounds were evaluated for their central nervous system (CNS) activity. Some of these compounds exhibited high activities in anti-pentylene tetrazole and rotarod test in mice orally administered.

Triazolyl ketone derivatives of the formula: STR1 (wherein R represents lower alkoxy or the group STR2 R4 and R5 each represents hydrogen, lower alkyl, STR3 represents hetero ring selected from pyrrolidino, piperidino, and morpholino; R1 represents halogen or nitro; R2 represents hydrogen or lower alkyl; R3 represents lower alkyl, phenyl, or the group STR4 R6 represents hydrogen, lower alkyl, or benzyl; R7 and R8 each represents hydrogen, lower alkyl, or STR5 represents hetero ring selected from pyrrolidino, piperidino, and morpholino; and Ar represents phenyl, o-halogenophenyl, or 2-pyridyl) and their pharmaceutically acceptable acid addition salts, being useful as anxiolytics, hypnotics, anticonvulsants, muscle relaxants, or their synthetic intermediates, are prepared by several routes.