| 摘要 |
<p>1382645 Derivatives of fused imidazoline ring systems BOEHRINGER INGELHEIM GmbH 14 April 1972 [15 April 1971] 17405/72 Heading C2C Novel compounds of the Formula I wherein R 1 and R 2 each represent hydrogen, halogen, C 1-3 alkyl, C 1 or C 2 alkoxy, cyano or trifluoro methyl, R 3 and R<SP>1</SP> 3 each represent hydrogen or hydroxy and n and m are zero or one and acid addition salts thereof may be prepared by (a) where at least one of n and m is 1 and at least one of R 3 and R<SP>1</SP> 3 is hydroxyl, hydrolysing or hydrogenating a compound V wherein R 4 and R<SP>1</SP> 4 are hydrogen, hydroxy or OZ where Z is a hydrolytically or hydrogenolytically removable protecting group, with the proviso that at least one of m and n is 1 and at least one of R 4 and R<SP>1</SP> 4 is OZ, (b) reacting a compound II with a compound XCH 2 (CHR 4 ) n (CHR<SP>1</SP> 4 ) m CH 2 Y, wherein X and Y are halogen, optionally isolating the intermediates IVa and/or IVb and where necessary effecting process (a); (e) reacting a compound VI with a compound XCH 2 CH 2 Y, optionally isolating the intermediates VIa and/or VIb and where necessary effecting process (a), (d) cyclizing the intermediates IVa, IVb, VIa, VIb formed by other processes, for example, by chlorinating the hydroxy group of 1-(2-hydroxy ethyl) - 2 - (2,6 - dichlorophenylamino) - imidazoline-(2). Pharmaceutical compositions of the compounds I decrease blood pressure when administered orally, parenterally or rectally with the usual excipients. Some of the compounds I also show analgesic, sedative and gastric juice secretion inhibiting activity.</p> |
