ORGN 133 |
Simple and convenient synthesis of coumarin-3-carboxamides
| N. Srinivasa Reddy, E. Premkumar Reddy, and M.V. Ramana Reddy. Fels Institute for Cancer Research, Temple University School of Medicine, 3307, North Broad Street, Philadelphia, PA 19140 |
The diverse biological activity of coumarin derivatives as anticoagulants, antithrombotics is well known in literature. Recently, some of the coumarin derivatives were also reported as antitumoral, anti-HIV, lipid-lowering agents. In particular, coumarin-3-carboxamides were reported as inhibitors of proteases, alfa-chymotrypsin (CT) and human leukocyte elastase (HLE). Here we wish to present a simple and convenient synthesis of coumarin-3-carboxamides, which we are now being evaluated for their biological activity. The title compounds were synthesized in one step by reacting substituted salicylaldehydes with N-aryl-malonamic acids in acetic acid using benzylamine as catalytic base. The pure products obtained in 60-80% yield after workout are screened for biological activity. |
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New Reactions and Methodology, Metal-Mediated Reactions, Heterocycles and Aromatics
8:00 PM-10:00 PM, Sunday, March 28, 2004 Anaheim Convention Center -- Hall A, Poster
Division of Organic Chemistry
The 227th ACS National Meeting, Anaheim, CA, March 28-April 1, 2004
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