Process for preparing triazolobenzodiazepines

Details Process for preparing triazolobenzodiazepines Process for preparing triazolobenzodiazepines

1977-01-24

1978-02-21

Rollins, Alton D.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

2602948B, 260296T, C07D48704

Patent

active

040752216

ABSTRACT:
An improved process for the production of 1-dialkyl-amino-ethyl-6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.2 is hydrogen, methyl or phenyl; wherein the ring A is unsubstituted, or monosubstituted with fluoro, chloro, bromo, nitro, trifluoromethyl or methylthio; and wherein Ar is phenyl; o-chlorophenyl; o-fluorophenyl; 2,6-difluorophenyl or 2-pyridyl, is carried out by reacting a compound of the Formula I: ##STR2## wherein ring A, Ar and R.sub.2 are defined as above, with a dialkylmethyleneammonium salt in the presence of a reactive carboxylic acylating agent.
The compounds of Formula II (R.sub.2 .dbd.H) are known compounds (Belgian Pat. No. 782,84g) which have sedative-tranquilizing as well as pronounced anti-depressant activity, suitable for the treatment of anxieties and depressions in mammals, including man.

REFERENCES:
patent: 4001262 (1977-01-01), Gall

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