A first synthesis of 18F-radiolabeled lapatinib: a potential tracer for positron emission tomographic imaging of ErbB1/ErbB2 tyrosine kinase activity

Fluorine-18-labeled lapatinib has been successfully synthesized for the first time by the reaction of a dimethylformamide solution of meta-[18F]fluorobenzylbromide with a Boc-protected lapatinib precursor fragment. The reaction proceeded in the presence of K2CO3 at 110 °C for 10 min in a microwave and was followed by Boc-group deprotection with trifluoroacetic acid. The overall radiochemical yield of the reaction starting from the radiofluorination of the iodonium salt was 8–12% (uncorrected, n = 6) in a 140-min synthesis time.