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

Basuli Falguni | Zendy; Wu Haitao | Zendy; Li Changhui | Zendy; Shi ZhenDan | Zendy; Sulima Agnieszka | Zendy; Griffiths Gary L. | Zendy

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

Author(s) -

Basuli Falguni,

Wu Haitao,

Li Changhui,

Shi ZhenDan,

Sulima Agnieszka,

Griffiths Gary L.

Publication year - 2011

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/jlcr.1898

Subject(s) - chemistry , lapatinib , trifluoroacetic acid , yield (engineering) , positron emission tomography , radiochemistry , pet imaging , chemical synthesis , medicinal chemistry , nuclear medicine , trastuzumab , organic chemistry , biochemistry , in vitro , breast cancer , medicine , materials science , cancer , metallurgy

Fluorine‐18‐labeled lapatinib has been successfully synthesized for the first time by the reaction of a dimethylformamide solution of meta ‐[ 18 F]fluorobenzylbromide with a Boc‐protected lapatinib precursor fragment. The reaction proceeded in the presence of K 2 CO 3 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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