| 摘要 |
1,178,434. Isoquinolobenzodiazepine derivatives preparation. F. HOFFMANN-LA ROCHE & CO. A.G. 20 Jan., 1967 [21 Jan., 1966], No. 3148/67. Heading C2C. Compounds of the general Formula I (R = halogen, CF 3 , NO 2 , NH 2 ; R<SP>1</SP> = alkyl, alkenyl, cycloalkylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl; R<SP>2</SP> = halogen, OH, NH 2 , alkyl, acyloxy, alkoxycarbonyl; R<SP>3</SP> = alkyl, alkoxycarbonyl; R<SP>4</SP> = alkyl; R<SP>5</SP> = halogen, CF 3 ; broken lines denote optional substituents) and their salts are prepared by reacting a compound of the Formula II (Y = NO 2 , NH 2 , alkyl-, alkenyl- or cycloalkylalkyl-substituted amino; C=N can be hydrogenated when Y= NO 2 ) with a compound of the Formula III (R<SP>20</SP> = alkyl, acyloxy, alkoxycarbonyl; R<SP>6</SP> = halogen, alkylsulphonyloxy, arylsulphonyloxy) or an amide, alkyl ester or aryl ester thereof where Y = NO 2 or an amide, alkyl ester, aryl ester, halide or anhydride thereof where Y = NH 2 or alkyl-, alkenyl- or cycloalkylalkylsubstituted amino, reducing any nitro value for Y, cyclizing any open-chain product obtained, if desired, introducing R<SP>1</SP> into the 5-position of the cyclization product and/or NO 2 , NH 2 or halogen into the 2-position thereof, if desired, hydrolysing any acyloxy group present and, if further desired, replacing the resulting OH group by halogen or NH 2 and, also if desired, converting any base obtained into a salt; the process including, where necessary, the reduction of any product containing a C=N bond. The preparation of 6,7,9,10-tetrahydro-6-oxo- 5H - isoquinolo - [2,1-d] - benzo - [1,4] - diazepinium bromide and chloride, 1-(2-acetamido- 5 - nitrophenyl) - 3,4 - dihydroisoquinoline, 1 - (2 - amino - 5 - nitrophenyl) - 3,4 - dihydroisoquinoline, 1 - (2 - bromoacetamido - 5 - nitrophenyl) - 3,4 - dihydroisoquinoline hydrobromide, 1 - (2 - (N - acetyl - N - methylamino) - 5 - nitrophenyl] - 3,4 - dihydroisoquinoline and 1 - (2 - methylamino - 5 - nitrophenyl) - 3,4 - dihydroisoquinoline is described. The compounds I and their salts are sedatives, tranquillizers, anticonvulsants and/or muscle relaxants, and may be administered in the form of pharmaceutical preparations containing them together with a carrier. |
