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METHOD OF SYNTHESIS OF 3-(1-THIAZOLIDINYLBUTYL-4-PIPERAZINYL)-1H-INDAZOLES

机译:3-(1-噻唑基丁基--4-哌嗪基)-1H-吲哚的合成方法

摘要

FIELD: organic chemistry. SUBSTANCE: product: 3-(1-thiazolidinylbutyl-4-piperazinyl)-1H-indazoles of the general formula (I) where R1 and R2 independently each of other hydrogen, lower alkyl or R1 and R2 together with carbon to which they are bound form cyclopentane or cyclohexane ring; R3 and R4 independently each of other hydrogen or lower alkyl; R5 hydrogen or lower alkyl; X hydrogen or halogen, or their pharmaceutically acid-additive salts. Reagent 1: derivative of 4-thiazolodinone of the formula (II) where R1, R2, R3 and R4 as indicated above. Reagent 2: 3-(1-piperazinyl)-1H-indazole of the formula (III) where X as indicated above. Reaction conditions: in the medium of organic solvent, at heating in atmosphere of inert gas. In the case of synthesis of compounds where R5 lower alkyl compound of the formula (I) where R3 hydrogen is alkylated. Synthesized compounds were used in medicine. EFFECT: improved method of synthesis. 1 tbl
机译:领域:有机化学。物质:产物:通式(I)的3-(1-噻唑烷基丁基-4-哌嗪基)-1H-吲唑,其中R 1 和R 2 彼此独立氢,低级烷基或R 1 和R 2 与它们所键合的碳一起形成环戊烷或环己烷环; R 3 和R 4 彼此独立地为氢或低级烷基; R 5 氢或低级烷基; X氢或卤素,或其药学上可加酸的盐。试剂1:式(II)的4-噻唑啉酮的衍生物,其中R 1 ,R 2 ,R 3 和R 4 如上所述。试剂2:式(III)的3-(1-哌嗪基)-1H-吲唑,其中X如上所述。反应条件:在有机溶剂介质中,在惰性气体气氛中加热。在合成其中R 3 氢被烷基化的式(I)的R 5 低级烷基化合物的化合物的情况下。合成的化合物用于医学。效果:改进的合成方法。 1汤匙

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