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analogifremgangsmåde for the manufacture of indolderivater or pharmaceutical acceptable syreadditionssalte thereof.
analogifremgangsmåde for the manufacture of indolderivater or pharmaceutical acceptable syreadditionssalte thereof.
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机译：用于制造吲哚美德或其药学上可接受的合成盐的类似物。
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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.
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机译：1318300吲哚衍生的酮和酮亚胺LABAZ 1971年11月22日[1970年12月9日]标题C2C本发明包括下式的化合物及其药学上可接受的酸加成盐，其中R 1是H，C 1-4烷基，环己基或Ph （可能被p-Cl，F或MeO取代）; R 2，R 5分别为H或C 1-4烷基; R 3为H，C 1-4烷基，Cl或MeO; R 4为H，C 1-4烷基或Cl; R 6为O或NH;和R 7为2-，3-或4-吡啶基（或其N-氧化物），条件是（a）当R 6为O时，R 7为吡啶基-N-氧化物，和（b）当R 6为NH时，R 2〜R 5各自为H，R 7为吡啶基，R 1不为Me。通过使相应的3-未取代的吲哚（II）与2-，3-或4-氰基吡啶或其N-氧化物反应来制备亚胺。通过（i）如上所述形成亚胺，然后水解，制备酮。 （ii）在路易斯酸的存在下使II与2-，3-或4-吡啶羧酸二烷基酰胺（N-氧化物）反应，并水解如此形成的配合物; （iii）使II-有机-Mg衍生物与2-，3-或4-吡啶羧酸卤化物（N-氧化物）反应，并水解如此形成的配合物。用于治疗炎症或抵抗血管内血栓形成的药物和兽医学组合物包含上述化合物（但条件不适用），并且可以口服，肠胃外，直肠或局部给药。
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