Facile synthesis of 2-perfluoroalkylated benzoxazolines and benzothiazolines

•An easy metal-free access to 2-perfluoroalkylated benzoxazolines and benzothiazolines.•The reaction was easily achieved under mild conditions in high yields and purity.•Study on the scope and regiochemistry of the reaction.•The protocol uses readily available methyl 2-perfluoroalkynoates as fluorine-containing building block.

The synthesis of 2-perfluoroalkylated benzoxazolines and benzothiazolines was easily achieved under mild conditions in high yields and purity. The protocol uses readily available methyl 2-perfluoroalkynoates as fluorine-containing building block, and furnished the expected product in good to excellent yields in MeOH under reflux for 10 h. This novel synthetic protocol is efficient and general. A plausible mechanism for this process is proposed.

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