- An indole derivative and its application
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The present invention relates to an indole derivative shown in formula (I-1) and its use in the preparation of a drug for the prevention and / or treatment of indications associated with the S1P receptor disorders. Indole derivatives of the present invent
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Paragraph 0113; 0115; 0120-0124
(2022/01/12)
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- Preparation method of 7-methyl indole
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The invention relates to a preparation method of 7-methyl indole. The preparation method comprises the following steps: (1) adding an organic solvent into a reaction kettle, heating, carrying out atmospheric distillation, adding a compound represented by formula (I), pyrrole and DMFDMA, carrying out reflux reaction, cooling, adding water and toluene into the reaction system, extracting, recoveringthe organic phase, drying with sodium sulfate, carrying out reduced pressure distillation to remove toluene, and drying to obtain an intermediate; and (2) adding the intermediate obtained in the step(1), an organic solvent and 5% Pd/C into a reaction kettle, carrying out normal-pressure hydrogenation and reflux reaction, carrying out diatomite suction filtration to remove Pd/C, carrying out vacuum concentration to obtain a brownish black oily liquid, adding water and ethyl acetate to extract a water phase, recovering an organic layer, washing with brine, drying with sodium sulfate, concentrating to dryness, and passing through a silica gel column to obtain white solid 7-methyl indole. The preparation method is simple, high in repeatability, stable in yield and suitable for large-scale production.
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Paragraph 0038; 0041-0042
(2021/03/11)
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- Studies on Several 7-Substituted N,N-Dimethyltryptamines
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Several 7-substituted derivatives of N,N-dimethyltryptamine (DMT) were prepared and evaluated in the rat fundus serotonin receptor assay and in a behavioral (discriminative stimulus) assay in rats.Both 7-Me- and 5-Ome-7-Me-DMT possess a higher pA2, and 5,7-(OMe)2-DMT a lower pA2, than that of DMT itself.Like DMT, all three of these compounds produce behavioral effects in rats which are similar to those of the hallucinogen 5-OMe-DMT.Although 7-Et- and 7-Br-DMT possess a higher serotonin receptor affinity than DMT, neither produce behavioral effects which parallelthose of 5-OMe-DMT.In contrast, 6-OMe-DMT and its 5-OMe derivative do not interact with the serotonin receptors in a competitive manner and are inactive in the discriminative stimulus assay.
- Glennon, R. A.,Schubert, E.,Jacyno, J. M.,Rosecrans, J. A.
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p. 1222 - 1226
(2007/10/02)
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