HPLC-free in situ18F-fluoromethylation of bioactive molecules by azidation and MTBD scavenging

Abstract

Sequential usage of azide and MTBD, which generates pure [¹⁸F]fluoromethyl tosylate and scavenges unreacted desmethyl precursors, provided an efficient HPLC-free strategy for the radiosynthesis of ¹⁸F-fluoromethylated compounds with high radiochemical yields and purity. This in situ¹⁸F-fluoromethylation can serve as a facile and efficient tool for the development of radiopharmaceuticals.