Inventors:
Michael Edward Derieg - Caldwell NJ
James Valentine Earley - Cedar Grove NJ
Rodney Ian Fryer - North Caldwell NJ
Leo Henryk Sternbach - Upper Montclair NJ
Assignee:
Hoffmann-La Roche Inc. - Nutley NJ
International Classification:
C07C 6996
Abstract:
Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. A bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. A bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. A are useful as sedative, muscle relaxant and anti-convulsant agents.