| 摘要 |
<p>Triazolobenzodiazepines of formula (I): (where R1 is 1-3C alkyl, R2 is 1-4C alkyl or -R2---R2 is a 2-5C divalent, saturated aliphatic hydrocarbon residue, and rings A and B may be substd. by F, Cl, Br, CF3, NO2, 1-6C alkyl or 1-6C alkoxy), e.g. 4-methyl-6-phenyl-8-chloro-4H-s-triazolo 4,3-a 1,4 benzodiazephine-1-carboxaldehyde diethylacetal, and their acid addn. salts are prepd. by reacting 2-X-3H-1,4-benzodiazepines (II)(where X is SH, NH2 or lower alkylamino, lower alkoxy or lower alkylthio opt. activated by a substituent) with a cpd. of the formula: in hexamethylphosphortriamide as solvent, the product being isolated as the base or as an acid addition salt. The product may be oxidised to give the corresp. 5-N-oxide, with H2O2 or a peracid. (I) and their 5-oxides have anticonvulsant, central depressant and muscle relaxant activity, and can be used as tranquilizers, sedatives, muscle relaxants and antiepileptics. 5-Oxides of (I) are also useful as intermediates for other pharmacologically active cpds.</p> |
