4.5 Article

Synthesis and Antiproliferative Activity of Polysubstituted Tetrahydropyridine and Piperidin-4-one-3-carboxylate Derivatives

Journal

ASIAN JOURNAL OF ORGANIC CHEMISTRY
Volume 1, Issue 1, Pages 71-79

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ajoc.201200010

Keywords

antiproliferation; multicomponent reactions; piperidin-4-ones; tetrahydropyridines; zirconium tetrachloride

Funding

  1. CSIR, New Delhi

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A highly atom-economic one-pot multicomponent synthesis of polysubstituted tetrahydropyridines (THPs) is described. The reaction of anilines, aromatic aldehydes, and beta-keto esters proceeds in the presence of catalytic amount of zirconium tetrachloride, and the products can be further converted to the corresponding piperidin-4-one-3-carboxylates under acidic conditions. The two sets of products were evaluated for their anticancer activity and some of these compounds, particularly the piperidin-4-one-3-carboxylates have significant anticancer activity.

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