1,5-Dihydro-7-aryl-as-triazine[4,3,-.alpha.][1,4]benzodiazepin-1

Details 1,5-Dihydro-7-aryl-as-triazine[4,3,-.alpha.][1,4]benzodiazepin-1 1,5-Dihydro-7-aryl-as-triazine[4,3,-.alpha.][1,4]benzodiazepin-1

1977-03-09

1978-04-25

Rollins, Alton D.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260239BD, 260296B, 2603407, 2603409R, 424244, 424249, 424278, A61K 3155, C07D40506, C07D48704

Patent

active

040862305

ABSTRACT:
Compounds of the formula: ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.2 is hydrogen, methyl or ethyl; wherein R.sub.3 is hydrogen, fluoro, chloro, bromo, nitro and -CF.sub.3 ; and wherein Ar is phenyl, o-chlorophenyl, o-fluorophenyl, 2,6-difluorophenyl, and 2-pyridyl, are prepared by treating a hydrazino compound of the formula: ##STR2## with a carbonyl compound II: ##STR3## wherein R.sub.1 is defined as above, and R', R" are alkyl of 1 to 3 carbon atoms, inclusive, or the group ##STR4## is a cyclic acetal, such as ##STR5## to give a compound of formula III: ##STR6## wherein R.sub.1, R.sub.2, R.sub.3, R', R" and Ar are defined as above, and cyclizing compound III to give the compound IV above.
Compounds III and IV, including the pharmacologically acceptable acid addition salt of these compounds, have sedative, anxiolytic and muscle-relaxing activity and can be used for the treatment of anxieties or muscle strains of mammals, including man.

REFERENCES:
patent: 3818003 (1974-06-01), Szmuszkovicz
patent: 3882112 (1975-05-01), Szmuszkovicz
patent: 3933816 (1976-01-01), Szmuszkovicz
patent: 4016165 (1977-04-01), Moffett
patent: 4017492 (1977-04-01), Moffett
patent: 4028356 (1977-06-01), Moffett
Moffett III, Letters on Heterocyclic Chemistry, vol. 3, pp. 3449-3456 (1976).

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