Practical synthesis of C-13-labeled conjugates by [C-13]CO-carbonylation of supported arylbipyridylpalladium complexes and alkyne-azide cycloadditions

A short procedure for the preparation of stable arylbipyridylpalladium complexes linked to a polystyrene resin is described. Starting from an o-iodobenzylalcohol with a pendant azido group, the corresponding supported complex was carbonylated with [C-13]CO to produce the desired C-13-labeled lactone tag with a satisfactory yield of 50%. This C-13-synthon was obtained with excellent purity after a simple filtration on sintered glass, and further conjugation using CuAAC and SPAAC reactions was performed with model substrates.