IMIDOZOLOBENZODIAZEPINES PROCESSES FOR THEIR PREPARATION AND COMPOSITIONS INCORPORATING THEM

摘要

1496426 1,2 - Dehydro - 6 - phenyl - 4H- imidazo [1,2 - a] [1,4] benzodiazepin - 1 - ones ROUSSEL LABORATORIES Ltd 13 Feb 1976 [15 Feb 1975 4 Nov 1975] 6509/75 and 45800/75 Headings C2C and C2P Novel compounds (I) and their acid addition salts in which R1 is H, Hal, NO 2 or CF 3 , R2 is H or Hal, R3 is H or Me and R4 and R5 are each H, C 1-5 alkyl, hydroxy C 1-5 alkyl or amino C 1-5 alkyl optionally mono- or di-C 1-5 alkylated or NR4R5 represents an optionally substituted heterocyclic ring optionally containing a further hetero atom are prepared by reacting a compound V with dimethylformamide C 1-5 acetal or dimethylacetamide and, if desired, transaminating the resultant product with an amine R4R5NH (where R4 and R5 are other than both Me). Compounds I (NR4R5 = piperazino) may be further reacted with a halide R6-Hal (where R6 is cycloalkyl alkyl, alkenyl or dialkylphosphenylalkyl) to form compounds I (NR4R5 = N-R6-piperazino). Compounds I are reacted with an acid to form the corresponding salt. Compounds V are prepared by cyclization of Compounds IV which are prepared by reacting a Compound II with a compound ROOC-CH 2 NH 2 , where R is an alkyl group. Compounds I have sedative, hypnotic, anxiolytic, tranquillizing, anticonvulsant and myorelaxant properties and form with a suitable vehicle a pharmaceutical composition which may be administered orally, parenterally or rectally.