- Observations concerning the synthesis of tryptamine homologues and branched tryptamine derivatives via the borrowing hydrogen process: Synthesis of psilocin, bufotenin, and serotonin
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Observations concerning the synthesis of substituted tryptamine derivatives starting from indoles and 1,n-amino alcohols via the borrowing hydrogen process are discussed. This catalytic, single-step, and modular approach to tryptamines and homotryptamines allows the synthesis of branched and nonbranched tryptamines as well as tryptamine-based natural products such as psilocin, bufotenin, and serotonin.
- Bartolucci, Silvia,Mari, Michele,Di Gregorio, Giovanni,Piersanti, Giovanni
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p. 2233 - 2238
(2016/04/19)
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- PIPERIDINE-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY
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Described herein are indole compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein, R is selected from the group consisting of H and C1-4alkyl; R is selected from the group consisting of H, C1-4alkyl and benzyl; -----
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Page/Page column 14
(2010/11/28)
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- Synthesis of pharmacologically relevant indoles with amine side chains via tandem hydroformylation/fischer indole synthesis
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The sequence of hydroformylation and Fischer indole synthesis starting from amino olefins and aryl hydrazines is described. In a convergent manner, the two units bearing pharmacologically relevant substituents are assembled in the final indolization step. This modular and diversity-oriented approach to tryptamines and homotryptamines can be conducted in water and allows synthesis of branched and nonbranched tryptamines as well as tryptamine-based pharmaceuticals such as the 5-HT1D agonist L 775 606.
- Schmidt, Axel M.,Eilbracht, Peter
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p. 5528 - 5535
(2007/10/03)
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- Piperidine-indole compounds having 5-HT6 affinity
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Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein: R1 is selected from the group consisting of H and C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; - - - represents a single or double bond; R3 is selected from the group consisting of COR5 and SO2R5; R4a is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4b is selected from the group consisting of H, hydroxy, halo, C3-7cycloalkyloxy, C1-4alkoxy, C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R4c is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4d is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; and R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C1-4alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C1-4alkylcarbonyl, C1-4alkoxycarbonyl and C1-4alkylS-. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
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