A first synthesis of 18F‐radiolabeled lapatinib: a potential tracer for positron emission tomographic imaging of ErbB1/ErbB2 tyrosine kinase activity |
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| Authors: | Falguni Basuli Haitao Wu Changhui Li Zhen‐Dan Shi Agnieszka Sulima Gary L Griffiths |
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| Institution: | Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, , Rockville, MD, 20850 USA |
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| Abstract: | 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. |
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| Keywords: | Radiolabeling Fluorine‐18 meta‐[18F]benzylbromide [18F]Lapatinib |
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