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A strain-induced copper-free click reaction mediated by a new and easily prepared cyclooctyne derivative was used to efficiently assemble a DOTA-biotin adduct capable of radionuclide ((68)Ga) uptake. This synthetic strategy offers a potentially general and convenient means of preparing targeted radiolabeling and radiotherapeutic agents.

Synthesis of a DOTA−Biotin Conjugate for Radionuclide Chelation via Cu-Free Click Chemistry