Synthesis of pharmacologically relevant indoles with amine side chains via tandem hydroformylation/Fischer indole synthesis |
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Authors: | Schmidt Axel M Eilbracht Peter |
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Institution: | Fachbereich Chemie, Organische Chemie I, Universit?t Dortmund, Otto-Hahn-Strasse 6, 44227 Dortmund. |
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Abstract: | reaction: see text] 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. |
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