7-Bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepine pharm

Details 7-Bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepine pharm 7-Bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepine pharm

1982-09-23

1985-03-19

Rollins, Alton D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

260239E, 260239BD, A61K 3155, C07D24316, C07D48704

Patent

active

045059080

ABSTRACT:
Disclosed are 7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines of the formula I ##STR1## in which R.sub.1 is a hydrogen atom or a lower alkoxy or alkanoyloxy radical and R.sub.2 is a halogen atom. The compounds possess psychopharmacological, and especially anti-aggressive properties. To manufacture compounds of formula I, corresponding 2-halomethyl-7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines are cyclized to corresponding 7-bromo-1,2-methylene-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines and in these the aziridine ring is opened through treatment with a lower alcohol or a lower carboxylic acid in the presence of a Lewis acid.

REFERENCES:
patent: 3998809 (1976-12-01), Milkowski et al.
patent: 4096141 (1978-06-01), Milkowski et al.
patent: 4098786 (1978-07-01), Milkowski et al.
patent: 4244869 (1981-01-01), Milkowski et al.

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