A process for the preparation of 4-[2-(Di-n-propylamino)ethyl]-2,3-dihydro-1H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formula I involving new intermediates of compound of formula (A) and (B) wherein R represents (i) a halogen atom selected from fluorine, chlorine atom, bromine atom and iodine atom; (ii) lower alkanesulfonyloxy group selected from methanesulfonyloxy, ethanesulfonyloxy, isopropanesulfonyloxy, propanesulfonyloxy, butanesulfonyloxy, tert-butanesulfonyloxy, pentanesulfonyloxy, hexanesulfonyloxy; (iii) substituted or unsubstantiated arylsulfonyloxy group selected from phenylsulfonyloxy, 4-methylphenylsulfonyloxy, 2-methylphenylsulfonyloxy, 4-nitrophenylsulfonyloxy, 4-methoxyphenylsulfonyloxy, 3-chlorophenylsulfonyloxy; (iv) arylalkylsulfonyloxy group selected from benzylsulfonyloxy, 2-phenylethylsulfonyloxy, 4-phenylbutylsulfonyloxy, 4-methylbenzylsulfonyloxy, 2-methylbenzylsulfonyloxy, 4-nitrobenzylsulfonyloxy, 4-methoxybenzylsulfonyloxy, 3-chlorobenzylsulfonyloxy.
一种制备式(I)的4-[2-(Di-n-propylamino)乙基]-2,3-二氢-1H-
吲哚-2-酮及其药学上可接受的盐、溶剂化合物的方法,其中式(I)涉及化合物式(A)和(B)的新中间体,其中R代表(i)从
氟、
氯、
溴和
碘中选择的卤素原子;(ii)从
甲烷基磺酰氧基、
乙烷基磺酰氧基、异丙基磺酰氧基、
丙烷磺酰氧基、丁磺酰氧基、叔丁磺酰氧基、戊磺酰氧基、己磺酰氧基中选择的低级烷基磺酰氧基;(iii)从苯基磺酰氧基、4-甲基苯基磺酰氧基、2-甲基苯基磺酰氧基、4-
硝基苯基磺酰氧基、4-
甲氧基苯基磺酰氧基、3-
氯苯基磺酰氧基中选择的取代或未取代芳基磺酰氧基;(iv)从苄基磺酰氧基、2-苯乙基磺酰氧基、4-苯基丁基磺酰氧基、4-甲基苯乙基磺酰氧基、2-甲基苯基磺酰氧基、4-
硝基苯基磺酰氧基、4-
甲氧基苯基磺酰氧基、3-
氯苯基磺酰氧基中选择的芳基烷基磺酰氧基。