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Synthesis and activity of conformationally rigidized N1-substituted-3-amino alkoxy indoles using intramolecular Heck reaction | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
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Abstract

Synthesis and activity of conformationally rigidized N1-substituted-3-amino alkoxy indoles using intramolecular Heck reaction

Author(s): Ramakrishna V. S. Nirogi1, Anand V. Daulatabad1, 2, Anil K. Shinde1*, K. R. Sastry1 and P. K. Dubey

A novel series of conformationally rigidized N1-substituted-3-aminoalkoxy indoles (tetracyclic derivatives) were designed and synthesized using intramolecular Heck cyclization in presence of tetrakis triphenyl phosphine palladium (0) catalyst. The compounds were characterized with spectral data and were tested for human 5-HT6 receptor binding affinities. All the compounds showed moderate binding affinities towards human 5-HT6 receptor.


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