A novel dibenzoazacyclooctyne precursor in regioselective copper-free click chemistry. An innovative 3-step synthesis

A novel carboxylic acid substituted dibenzoazacyclooctyne precursor has been synthesized using a fast and innovative three-step synthesis. It can be easily converted into the corresponding alkyne through UV-irradiation. Due to its fast and regioselective reaction with azides, the alkyne is a promising agent for copper-free click chemistry. The second order reaction rate constant was determined by H-1-NMR.