Synthesis of a DOTA-biotin conjugate for radionuclide chelation via Cu-free click chemistry

Abstract

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 (68Ga) uptake. This synthetic strategy offers a potentially general and convenient means of preparing targeted radiolabeling and radiotherapeutic agents. © 2010 American Chemical Society.