Betts Helen M, Robins Edward G
GE Healthcare Discovery, Medical Diagnostics, Cyclotron Building, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK; GE Healthcare Discovery, Medical Diagnostics, The Grove Centre, White Lion Road, Amersham, Bucks, HP7 9LL, UK; Nottingham University Hospitals NHS Trust, PET/CT Centre, Nottingham City Hospital, Nottingham, NG5 1PB, UK.
J Labelled Comp Radiopharm. 2014 Apr;57(4):215-8. doi: 10.1002/jlcr.3147. Epub 2013 Dec 18.
Novel radiolabelling methods are important for the development of new tracers for positron emission tomography. Direct nucleophilic fluorination of aromatic rings with [(18) F]fluoride is limited to activated substrates, restricting the application of this approach. Inspired by transition metal-mediated transformations, a fluorine-18 synthon was prepared to supplement the radiolabelling methods available for molecules unsuitable for direct labelling. 2-Bromo-6-[(18) F]fluoropyridine (denoted [(18) F]1) was prepared in high yield, and palladium-mediated cross-coupling reactions were exemplified. High incorporation of fluoride and efficient cross-coupling reactions demonstrate that compound [(18) F]1 holds promise as a new synthon for construction of fluorine-18-labelled molecules via transition metal-mediated reactions.
新型放射性标记方法对于正电子发射断层扫描新示踪剂的开发至关重要。用[¹⁸F]氟化物对芳环进行直接亲核氟化仅限于活性底物，限制了该方法的应用。受过渡金属介导的转化反应启发，制备了一种¹⁸F合成子，以补充适用于不适于直接标记的分子的放射性标记方法。以高产率制备了2-溴-6-[¹⁸F]氟吡啶（表示为[¹⁸F]1），并举例说明了钯介导的交叉偶联反应。高氟掺入率和高效的交叉偶联反应表明，化合物[¹⁸F]1有望成为通过过渡金属介导的反应构建¹⁸F标记分子的新型合成子。
