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One‐Pot Decarboxylative Acylation of N‐, O‐, S‐Nucleophiles and Peptides with 2,2‐Disubstituted Malonic Acids |
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| Authors: | Dr Iryna O Lebedyeva Dr Suvendu Biswas Kevin Goncalves Sean M Sileno Ashton R Jackson Kunal Patel Prof Dr Peter J Steel the late Prof Dr Alan R Katritzky |
| Institution: | 1. Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611‐7200 (USA), Fax: (+1)?352‐392‐9199;2. Department of Chemistry and Physics, Georgia Regents University, 1120 15th Street SCI W3005, Augusta, GA 30912 (USA);3. Department of Chemistry, University of Canterbury, Christchurch 8140 (New Zealand) |
| Abstract: | Monocarbonyl activation of 2,2‐disubstituted malonic acids with benzotriazole leads to decarboxylation of one of the carboxy groups and formation of a C?H bond. Intermediate carbonyl benzotriazoles then readily acylate nucleophilic reagents and peptides resulting in libraries of conjugates and peptidomimetics. |
| Keywords: | acylation cleavage reactions conjugates decarboxylation peptides |