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

作者：Basuli Falguni; Wu Haitao; Li Changhui; Shi Zhen Dan; Sulima Agnieszka; Griffiths Gary L^*

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2011, 54(9-10): 633-636.

DOI：10.1002/jlcr.1898

• Radiolabeling
• Fluorine-18
• meta-[F-18]benzylbromide
• [F-18]Lapatinib

Fluorine-18-labeled lapatinib has been successfully synthesized for the first time by the reaction of a dimethylformamide solution of meta-[F-18]fluorobenzylbromide with a Boc-protected lapatinib precursor fragment. The reaction proceeded in the presence of K2CO3 at 110 degrees 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.

• 出版日期2011-8
• 单位NIH