Organomediated cleavage of benzoyl group enables an efficient synthesis of 1-(6-nitropyridin-2-yl)thiourea and its application for developing 18F-labeled PET tracers

The efficient synthesis of 1-(6-nitropyridin-2-yl)thiourea was developed under mild reaction conditions, which previously has been challenging to prepare by conventional methods due to the highly reactive nature of the ortho-nitro group on the pyridine ring. This method permits the development of various 18F labeled heterocycles as PET imaging ligands such as N-(pyridin-2-yl)thiazol-2-amine derivatives. The feasibility of this approach was demonstrated by the synthesis of a 18F-labeled PET tracer for studying prion disease.