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The selective halocyclization and iodosulfonylation of N-benzothiazol-2-yl alkynamides under mild conditions is described. An effective synthetic strategy to pyrimidobenzothiazoles via a 6-endo-dig halocyclization of N-benzothiazol-2-yl alkynamides was developed at room temperature with a broad substrate scope. Furthermore, several multisubstituted α,β-enones were synthesized using the same starting materials.

Graphical abstract: Selective halocyclization and iodosulfonylation of N-benzothiazol-2-yl alkynamides under mild conditions

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