- A PRACTICAL AND SHORT ACCES TO 4-HYDROXY-3-INDOLECARBALDEHYDE AND ITS APPLICATION FOR THE SYNTHESIS OF PINDOLOL ANALOG
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4-Hydroxy-3-indolecarbaldehyde (1) is produced simply by heating (3-formylindol-4-yl)thallium bis-trifluoroacetate with copper sulfate in N,N-dimethylformamide and water.Alkylation of 1 afforded predominantly 1-alkyl derivatives.Utilizing these results pindolol analog, 1-allyl-4-(3-t-butylamino-2-hydroxypropoxy)-3-indolecarbaldehyde was synthesized.
- Somei, Masanori,Iwasa, Etsuo,Yamada, Fumio
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- Tricylic indole compounds having affinity for serotonin receptor
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Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems. (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ═O or ═S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on)
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- TRICYCLIC INDOLE COMPOUNDS HAVING AFFINITY FOR SEROTONIN RECEPTOR
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Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems. (wherein R1 is hydrogen ; R2 is hydrogen or lower alkyl ; R
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- Synthetic studies of psilocin analogs having either a formyl group or bromine atom at the 5- or 7-position.
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Psilocin analogs having either a formyl group (9-12) or a bromine atom (13-18) at the 5- or 7-position have been prepared for the first time. Syntheses of 5- and 7-bromo derivatives of 4-hydroxy- (23, 24, 28) and 4-benzyloxyindole-3-carbaldehyde (19, 25,
- Yamada, Fumio,Tamura, Mayumi,Hasegawa, Atsuko,Somei, Masanori
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- Preparations of 1-hydroxyindole derivatives and their potent inhibitory activities on platelet aggregation
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1-Hydroxymelatonin, 5-bromo- and 5,7-dibromo-1-hydroxytryptamine derivatives, 1,4-dihydroxy-5-nitroindole, 1-hydroxy-3-methylsulfinylmethylindole, and 5-acetyl-1,3,4,5-tetrahydro-1-hydroxypyrrolo[4,3,2-de]quinoline were synthesized for the first time. 1-Hydroxyindoles revealed potent inhibitory activities on platelet aggregation.
- Somei, Masanori,Yamada, Koji,Hasegawa, Masakazu,Tabata, Mutsuko,Nagahama, Yoshiyuki,Morikawa, Harunobu,Yamada, Fumio
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p. 1855 - 1858
(2007/10/03)
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- 3-Cyano indoles as intermediates for cardioselective compounds
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The present invention provides indole derivatives of the general formula: STR1 wherein R1 is a hydrogen atom, an aralkyl radical or a radical of the general formula: STR2 in which B is a reactive group or, together with R5, represent
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