A series of regioselective methods to access fully substituted 4-sulfonyl, 4-phosphonates- and 5-amido-, 5-sulfonyl-, 5-trifluoromethylthio-, 5-thio-1,2,3-triazoles from the internal alkynes by transition metal-catalyzed azide-alkyne cycloaddition (MAAC) reaction under mild conditions have been developed. These approaches feature good compatibility with water and air, broad substrate scopes, good functional group tolerance, high yields and excellent regioselectivities. The advantages of this method further include its applicability to gram-scale preparation, the use of solid-phase synthesis technique, and the mutually orthogonal CuAAC-RhAAC reaction and so on.

Transition metal-catalyzed highly regioselective azide-internal alkynes cycloaddition under mild conditions

2019 Fall National Meeting

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