✦ LIBER ✦
A first synthesis of 18F-radiolabeled lapatinib: a potential tracer for positron emission tomographic imaging of ErbB1/ErbB2 tyrosine kinase activity
✍ Scribed by Falguni Basuli; Haitao Wu; Changhui Li; Zhen-Dan Shi; Agnieszka Sulima; Gary L. Griffiths
- Publisher
- John Wiley and Sons
- Year
- 2011
- Tongue
- French
- Weight
- 596 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
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.