| 摘要 |
<p>1-(2-alkyl aminoethyl)-S-triazolo (4,3-a) (1,4) benzodiazepines (VIII) are prepared by treating 2-hydrazino (1,4)benzodiazepines (V) with a beta-phthalimidoalkanoic acid and a dehydrating agent to give 1-(2-phthalimidoethyl)-S-triazolo (4,3-a) (1,4),benzodiazepines (VI). These are then reacted with hydrazine in ethanol to give 1-(2-aminoethyl)-S-triazolo (4,3-a) (1,4)benzodiazepines (VII) which are alkylated with a carboxylic acid aldehyde to give (VIII). In the formulae R=H, methyl or ethyl; R' and R" = H or (1-3C) alkyl, at least one is alkyl; R1 = H or methyl; R2,R3,R4 and R5=H, (1-3C)alkyl, halogen, NO2CF3, (1-3C) alkoxy or (1-3C)alkylthio). The product (VIII) may be further reduced to the 6,7-dihydro deriv. (IX) with diborane. Compounds (VIII) and (IX) and their acid addn. salt are sedatives, tranquillisers, muscle relaxants and antidepressants. Preparation of 1-(2-(di-methylamino)ethyl)-8-chloro-6-phenyl-4H-s-triazolo (4,3-a) (1,4)benzodiazepine is disclosed.</p> |
