• Open Access

Thiacycloalkynes for Copper-Free Click Chemistry


  • E.M.S. was supported by a predoctoral fellowship from the American Chemical Society Division of Organic Chemistry (Genentech). H.N. was partially supported by the Amgen Scholars Program. This work was supported by a grant to C.R.B. from the NIH (GM58867).


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The heteroatom helps! The introduction of an endocyclic sulfur atom enables fine-tuning of the reactivity and stability of thiacycloalkynes for copper-free click chemistry. The stabilizing effect of the endocyclic sulfur atom allows the use of highly activated seven-membered rings as reagents for bioorthogonal copper-free click chemistry.