| 摘要 |
<p>1,198,703. Benzodiazepine derivatives. F. HOFFMANN-LA ROCHE & CO. A.G. 22 Nov., 1967 [23 Nov., 1966], No. 53100/67. Heading C2C. Compounds of the general formula (R<SP>1,2</SP>=optional halogen, CF 3 , NO 2 , C 1-6 alkyl, NH 2 , CN; R<SP>3</SP> = optional C 1-6 alkyl; R<SP>4</SP> = phenyl, halophenyl, pyridyl; A = dimethylene or trimethylene which may carry a C 1-6 alkyl substituent on one or more of its carbon atoms) and their acid addition and quaternary salts are prepared by heating a compound (which may be prepared in situ) of the formula (n = 0 or 1; R<SP>5</SP>'<SP>6,7</SP> = optional C 2-6 alkyl), optionally followed by one or more of the steps: (a) conversion of an N-oxide to the desoxy compound, (b) nitration, (c) reduction of NO 2 to NH 2 , (d) replacement of NH 2 by halogen or CN, (e) salt formation. The starting materials may be prepared by (a) reacting a compound of the formula (hal = halogen) with NH 3 or (b) solvolysing a compound of the formula (X = carbobenzoxyamino, phthalimido, succinimido, alkanoylamino). The compounds of the two latter general formulµ may be prepared from the corresponding 1-unsubstituted benzodiazepine derivative. The compounds of the invention are anticonvulsants, muscle relaxants, psychostimulants and sedatives and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier.</p> |
