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    • 4. 发明申请
    • PROCESS FOR THE PREPARATION OF INDOLONE DERIVATIVE
    • 制备吲哚酚衍生物的方法
    • WO2006123356A1
    • 2006-11-23
    • PCT/IN2006/000052
    • 2006-02-15
    • ALEMBIC LIMITEDSONI, Rohit, RavikantACHARYA, Hitarth, HarshenduSHAH, Hetal, RameshchandraSHAH, Trushar, RajnikantREDDY, Buchi, Reguri
    • SONI, Rohit, RavikantACHARYA, Hitarth, HarshenduSHAH, Hetal, RameshchandraSHAH, Trushar, RajnikantREDDY, Buchi, Reguri
    • C07D207/26
    • C07D207/26
    • A process for the preparation of 4-[2-(Di-n-propylamino) ethyl]-2,3-dihydro-1 H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formaula 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.
    • 制备式(I)的4- [2-(二正丙基氨基)乙基] -2,3-二氢-1H-吲哚-2-酮及其药学上可接受的盐,溶剂合物的方法涉及 式(A)和(B)化合物的新中间体,其中R表示(i)选自氟,氯原子,溴原子和碘原子的卤素原子; (ii)选自甲磺酰氧基,乙磺酰氧基,异丙磺酰氧基,丙磺酰氧基,丁磺酰氧基,叔丁磺酰氧基,戊磺酰氧基,己磺酰氧基等低级烷磺酰氧基。 (iii)选自苯基磺酰氧基,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-氯苯基磺酰氧基等的取代或未经取代的芳基磺酰氧基; (iv)选自苄基磺酰氧基,2-苯基乙基磺酰氧基,4-苯基丁基磺酰氧基,4-甲基苄基磺酰氧基,2-甲基苄基磺酰氧基,4-硝基苄基磺酰氧基,4-甲氧基苄基磺酰氧基,3-氯苄基磺酰氧基的芳烷基磺酰氧基。