| abstract |
NOVEL BENZODIAZEPINES REPRESENTED BY THE FORMULA, 1-(R4-(-O-)>CH-CNH2N-),2-(O=),3-R3,5-R2,R1-1,2-DIHYDRO- 3H-1,4-BENZODIAZEPINE WHEREIN R1 REPRESENTS HYDROGEN, HALOGEN, NITRO, C1-4 ALKOXY, CYANO OR TRIFLUOROMETHYL; R2 REPRESENTS A GROUP OF THE FORMULA, (PYRIDYL)-, OR (R5,R6-BENZENE) (WHEREIN R5 AND R6 REPRESENT HYDROGEN, HALOGEN, TRIFLUOROMETHYL, CYANO OR C1-4 ALKY); R3 AND R4 REPRESENT HYDROGEN OR C1-4 ALKYL; AND N REPRESENTS AN INTEGER OF 1 TO 4 ARE PREPARED BY REACTING A 1-UNSUBSTITUTED BENZODIAZEPINE REPRESENTED BY THE FORMULA, 2-(O=),3-R3,5-R2,R1-1,2-DIHYDRO-3H-1,4-BENZODIAZEPINE WHEREIN R1, R2 AND R3 ARE AS DEFINED ABOVE, WITH A REACTIVE ESTER OF ALCOHOL REPRESENTED BY THE FORMULA HO-CNH2N-CH<(-O-)(-R4) WHEREIN R4 IS AS DEFINED ABOVE. RHE BENZODIAZEPINE DERIVATIVES OF THE FORMULA I HAVE VALUABLE PHARMACOLOGICAL PROPERTIES, IN PARTICULAR EXCELLENT TRANQUILIZING, SEDATIVE, MUSCLE RELAXANT, ANTICONVULSANT AND HEXOBARBITAL POTENTIATING ACTIVITIES. |