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METHOD FOR SYNTHESIS OF ISOINDOLINONE DERIVATIVES OR THEIR SALTS

机译:异吲哚啉酮衍生物或其盐的合成方法

摘要

Compounds of formula: IMAGE (I) in which: either R1 represents 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl or 4-(4-fluorophenyl)-1,2,3,6-tetrahydro-1-pyridyl, R2 represents hydrogen, alkoxy of 1 or 2 carbon atoms, hydroxyl, alkyl, alkylthio, alkylcarbonyloxy, phenylalkylcarbonyloxy, phenylalkyl or -NR4R5 in which R4 represents hydrogen or alkyl and R5 represents alkyl, phenyl, monohalogenated phenyl or pyridyl, and R3 represents a hydrogen atom, or else R2 represent phenyl and R3 represents hydrogen or hydroxyl; or R1 represnets 4-phenyl-1-piperazinyl whose phenyl nucleus has a substituent halogen atom or hydroxyl radical in the 4-position, R2 represents alkoxy and R3 represents hydrogen; it being understood that when R1 represents the 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl radical, R2 is not hydroxyl and that, unless otherwise stated, the alkyl and alkoxy radicals and the alkyl and alkoxy portions contain 1 to 4 carbon atoms each in a straight or branched chain, and addition salts thereof with an inorganic or organic acid, are useful in therapy for their serotonin antagonist properties.
机译:式:(I)的化合物,其中:R1代表4-苯基-1,2,3,6-四氢-1-吡啶基或4-(4-氟苯基)-1,2,3,6-四氢-1-吡啶基,R2代表氢,1或2个碳原子的烷氧基,羟基,烷基,烷硫基,烷基羰氧基,苯基烷基羰氧基,苯基烷基或-NR4R5,其中R4代表氢或烷基,R5代表烷基,苯基,单卤代苯基或吡啶基,并且R 3代表氢原子,或者R 2代表苯基并且R 3代表氢或羟基; R1代表苯基核在4位上具有取代基卤原子或羟基的4-苯基-1-哌嗪基,R2表示烷氧基,R3表示氢。应当理解,当R 1代表4-苯基-1,2,3,6-四氢-1-吡啶基时,R 2不是羟基,并且除非另有说明,否则烷基和烷氧基以及烷基和烷氧基部分包含直链或支链中的每个有1-4个碳原子,以及它们与无机或有机酸的加成盐,由于其5-羟色胺拮抗剂的特性而可用于治疗。

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