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Synfacts 2011(12): 1367-1367
DOI: 10.1055/s-0031-1289381
DOI: 10.1055/s-0031-1289381
Organo- and Biocatalysis
© Georg Thieme Verlag
Stuttgart ˙ New York
Organo-Click Synthesis of 1,2,3-Triazoles from Unactivated Ketones
M. Belkheira, D. El Abed, J.-M. Pons*, C. Bressy*
Aix-Marseille Université, France and Université d’Oran Es-Sénia, Algérie
Further Information
Publication History
Publication Date:
18 November 2011 (online)
Significance
Bressy, Pons and co-workers have developed a new route to highly substituted 1,2,3-triazoles starting from unactivated ketones and arylazides with good regio- and chemoselectivity. Proline was established as an excellent organocatalyst for this reaction, with the acid moiety being crucial for the elimination step via intermediate A. A dramatic acceleration of the reaction rate was observed when using microwave activation.