| 摘要 |
1318300 Indole-derived ketones and ketimines LABAZ 22 Nov 1971 [9 Dec 1970] 58543/70 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts, wherein R 1 is H, C 1-4 alkyl, cyclohexyl or Ph (possibly p-Cl, F or MeO- substituted); R 2 , R 5 are each H or C 1-4 alkyl; R 3 is H, C 1-4 alkyl, Cl or MeO; R 4 is H, C 1-4 alkyl or Cl; R 6 is O or NH; and R 7 is 2-, 3- or 4-pyridyl (or their N-oxides), provided that (a) when R 6 is O, R 7 is pyridyl-N-oxide, and (b) when R 6 is NH, R 2 ... R 5 are each H and R 7 is pyridyl, R 1 is not Me. The imines are prepared by reacting the corresponding 3-unsubstituted indole (II) with 2-, 3- or 4-cyanopyridine or its N-oxide. The ketones are prepared by (i) forming the imine as just described, followed by hydrolysis; (ii) reacting II with a 2-, 3- or 4- pyridinecarboxylic acid dialkylamide (N-oxide) in presence of a Lewis Acid, and hydrolysing the complex so formed; (iii) reacting II-organo-Mg derivative with a 2-, 3- or 4-pyridinecarboxylic acid halide (N-oxide), and hydrolysing the complex so formed. Pharmaceutical and veterinary compositions for treating inflammation or combatting intravascular thrombosis comprise the above compounds (but the proviso does not apply), and may be administered orally, parenterally, rectally or topically. |
