| 摘要 |
1391828 Oxindole derivatives SANDOZ Ltd 20 June 1972 [24 June 1971 (3)] 28744/72 Heading C2C Novel compounds of Formula I wherein R 1 is hydrogen or alkyl of 1 to 4 carbon atoms, R 2 is alkyl of 1 to 6 carbon atoms; cycloalkyi of 3 to 8 carbon atoms; alkoxyalkyl of 3 to 10 carbon atoms, the oxygen atom thereof being separated from the nitrogen atom by at least 2 carbon atoms; phenylalkyl of 8 to 12 carbon atoms, the phenyl being separated from the nitrogen atom by at least 2 carbon atoms; phenylalkyl of 8 to 12 carbon atoms mono-substituted on the phenyl ring by alkyl of 1 to 5 carbon atoms or alkoxy of 1 to 5 carbon atoms, the phenyl being separated from the nitrogen atom by at least 2 carbon atoms; alkynyl of 2 to 7 carbon atoms; or carbalkoxyalkyi, the alkoxy substituent thereof having 1 to 4 carbon atoms and the alkyl substituent thereof having 1 to 6 carbon atoms; R 3 is hydrogen; or -COA, wherein A is alkyl or 1 to 12 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms substituted by alkyl of 1 to 4 carbon atoms, or a 5- or 6-membered oxygen-containing heterocycle; and the aminopropoxy side chain is in the 4 or 7 position of the oxindole nucleus, and acid addition salts thereof, are prepared either by reacting a compound of Formula III with the amine H 2 NR 2 and optionally acylating the resulting alcohol or (b) debenzylating a compound of Formula V wherein R<SP>1</SP> 2 is as R 2 except it may not be alkynyl or carbalkoxyalkyl and in both cases forming acid addition salts if required. 4- (2.3-Epoxypropoxy)oxindole is prepared from 4-hydroxy-oxindole and epibromohydrin. Pharmaceutical compositions in conventional forms for oral administration having a #- blocking action comprise an above novel compound and a carrier or diluent therefor. |
