Tandem Oxidative alpha-Tosyloxylation of Alcohols/Nucleophilic Addition of Azide/Copper-Catalyzed 1,3-Dipolar Cycloaddition

[摘要]：An efficient method is described for the regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles (beta-keto-1,2,3-triazoles) in good to excellent yields by the successive treatment of secondary alcohols with [hydroxy(tosyloxy) iodo]benzene (Koser's reagent, HTIB), sodium azide followed by copper(I) iodide catalyzed 1,3-dipolar cycloaddition with terminal alkynes.

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