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

Abstract

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 [13C]CO to produce the desired 13C‐labeled lactone tag with a satisfactory yield of 50%. This 13C‐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.