| 摘要 |
The invention comprises compounds of the general formula <FORM:0991937/C2/1> (wherein R represents a hydrogen or halogen atom, R1 represents a hydrogen atom or a methyl group, and R2 and R3 represent hydrogen atoms or C1-4 alkyl groups or, together with the nitrogen atom, form an indoline ring which may be halogenated in the 5-position, or a saturated 5- or 6-membered heterocyclic ring) and physiologically tolerable acid addition salts thereof, pharmaceutical preparations containing them, and their preparation by known methods, e.g. from indoline or a 5-haloindoline. The following intermediates are prepared from the starting materials indicated in parentheses: 1 - crotonylindoline (indoline and crotonyl chloride); 1-(b -ethylaminocrotonyl)-indoline (indoline and diketene, via 1-acetoacetylindoline); 1 - crotonyl - 5 - fluoroindoline - (5-fluoroindole, via 5-fluoroindoline); 1-(b -methylcrotonyl)-indoline (indoline and b -methylcrotonyl chloride); b -bromoisovaleryl chloride (b -bromoisovaleric acid); 1-(b -methylcrotonyl)-5-bromoindoline (1 - acetyl - 5 - bromoindoline, via 5 - bromoindoline); b - bromobutyryl chloride (b -bromobutyric acid); 1-(b -bromobutyryl) - indoline (1 - acetoacetylindoline or 1 - acetoacetylindole, via 1 - (b - hydroxybutyryl)-indoline, or indoline and b -bromobutyryl chloride). The compounds of the invention have sympathicolytic activity and lower the blood pressure; they may be administered orally or parenterally in the form of pharmaceutical preparations (e.g. tablets, dragees and sterile aqueous solutions) containing them in admixture or conjunction with a carrier. |
