| 摘要 |
<p>Benzodiazepines of formula (I) and the 5-N-oxides (where R1 = H or a hydrocarbon residue, e.g. (1-6C) alkyl, (7-8C) aralkyl or aryl, R2 = H or alkyl, and rings A and/or B may be substd. by one or more NO2, CF3, hal., alkyl or alkoxy), are of use as muscle relaxants, anticonvulsants, sedatives and tranquillisers, at a dose of 1-30 mg./d. (p.o.), or 0.5-10 mg/d. (parenteral). (I) are prepd. by reaction of the novel hydrazides (II) with a carboxylic acid R'CO2H (III) or its reaction deriv. Sedative chloro-phenyl-triazolobenzodiazepines.. followed by ring closure if necessary. The reaction is carried out with 1-10 mol. (III) at 0-300 degrees in the presence of an acid catalyst. (II) are prepd. from the corresp. amine, alkylthio or aralkylthio deriv. and N2H4.</p> |
