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A facile synthetic method to access 4-amino-isoquinolin-1(2H)-one and oxazole derivatives was disclosed in this paper. The reaction of N-(pivaloyloxy)-amides with ynamides produced 4-amino-isoquinolin-1(2H)-ones in good yields in the presence of Cp*Rh(III) catalyst through a C–H bond functionalization. Using Sc(OTf)3 as the catalyst, oxazole derivatives were obtained in good yields from the same reaction. This protocol features good functional group tolerance and excellent regioselectivity.

Graphical abstract: Catalyst-controlled synthesis of 4-amino-isoquinolin-1(2H)-one and oxazole derivatives

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