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One-Pot Two-Component [3 + 2] Cycloaddition/Annulation Protocol for the Synthesis of Highly Functionalized Thiophene Derivatives

Ganesh Chandra Nandi, Subhasis Samai and Maya Shankar Singh*

*Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi-221005, India, Email:

G. C. Nandi, S. Samai, M. S. Singh, J. Org. Chem., 2011, 76, 8009-8014.

DOI: 10.1021/jo200685e (free Supporting Information)


4-dimethylaminopyridine (DMAP) promotes an efficient and experimentally rapid protocol for the synthesis of 2,3-dicarboalkoxy-4-aroyl/heteroaroyl/alkanoyl thiophenes in high yields via 1-2 (C-S) and 3-4 (C-C) bond connections in only 3-5 min in DCM at room temperature. This method allows a clean and general synthesis of previously inaccessible and synthetically demanding thiophenes.

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ID: J42-Y2011-2920