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The novel compounds of spiro indole - ethyl agonists of melatonin, a process for their preparation and their use as a medicinal product.

机译:褪黑激素的螺[吲哚-乙基]激动剂的新型化合物,其制备方法及其用作药物的用途。

摘要

Spiro(3H- indol- 3(2H),3'-pyrrolidine) derivs. of formula (I) and their racemates, pure enantiomers (or mixts. in all proportions) and salts are new. In (I), X-Y partial bond is -N=CR6- (cpds. (Ia)) or -N(COR1)-CH(OCOR1)- (cpds. (Ib)); R1 is H, lower alkyl, aryl or lower aralkyl (all opt. substd. by one or more halo) or lower perhaloalkyl; R2-R5 are H, OH, lower alkyl, lower alkoxy, aryloxy, lower aralkoxy, halo or NO2; R6 is H, lower alkyl, aryl, lower aralkyl, lower alkoxy or halo. All lower alkyl moieties have 1-6 C atoms. Also new are 1'-unsubstd. spiro(indole-pyrrolidine) intermediates of formula (IV).
机译:Spiro(3H-吲哚-3(2H),3'-吡咯烷)衍生。式(I)的化合物,其外消旋体,纯对映异构体(或所有比例的混合物)和盐是新的。在(I)中,X-Y部分键为-N = CR 6-(cpds。(Ia))或-N(COR1)-CH(OCOR1)-(cpds。(Ib)); R 1是H,低级烷基,芳基或低级芳烷基(均被一个或多个卤素取代)或低级全卤代烷基; R 2 -R 5是H,OH,低级烷基,低级烷氧基,芳氧基,低级芳烷氧基,卤素或NO 2; R 6是H,低级烷基,芳基,低级芳烷基,低级烷氧基或卤素。所有低级烷基部分均具有1-6个碳原子。 1'-unsubdd也很新。式(IV)的螺(吲哚-吡咯烷)中间体。

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