| 摘要 |
1285529 Benzodiazepines HOFFMANN LA ROCHE & CO AG 27 July 1971 [29 July 1970] 35138/71 Heading C2C Compounds of the general Formula (I) (R<SP>1</SP> = halogen, N0 2 ; R<SP>2</SP> = Ph, Py, halophenyl; R<SP>3</SP> = alkoxy; R<SP>4</SP> = haloalkyl, alkoxyalkyl, carboxyalkyl, alkylamino, dialkylamino, R<SP>6</SP>R<SP>7</SP>N-alkyl (R<SP>6</SP>'<SP>7</SP> = H, alkyl or NR<SP>6</SP>R<SP>7</SP> = 5-6 membered saturated ring optionally containing an O atom), optionally substituted 5-6 membered aromatic ring containing 1-2 heteroatoms; n = 0, 1) and their salts are prepared by (a) acylating the corresponding primary alcohol, (b) replacing the side-chain halogen atom in a compound of the Formula (IV) by OCOR<SP>8</SP> (R<SP>8</SP> = haloalkyl, alkoxyalkyl, R<SP>6</SP>R<SP>7</SP>N.alkyl, optionally substituted 5-6 membered aromatic ring containing 1-2 heteroatoms), (c) reacting a compound of the Formula (VI) (R<SP>9</SP> = alkyl substituted by leaving atom or group) with R<SP>6</SP>R<SP>7</SP>NH, (d) cyclizing a compound of the Formula (VIII) (e) oxidizing a compound of Formula (I), n = O, (f) deoxygenating a compound of Formula (I), n = 1, (g) dehydrating a compound of the Formula (IX) (h) oxidizing or dehydrogenating a compound of the Formula (X) (i) treating a compound of the Formula (XI) (R<SP>10</SP> = acyl) with a base, (j) treating a compound of the Formula (XII) (R<SP>11</SP> = alkylsulphonyl, arylsulphonyl) with a strong base or (k) rearranging a compound of the Formula (XIII) optionally followed in each case by salt formation. The preparation of starting materials for processes (a) and (b) is described. The above compounds are anticonvulsants, muscle relaxants, sedatives and anxiolytics and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier. |
