作者:Katarina J. Makaravage、Allen F. Brooks、Andrew V. Mossine、Melanie S. Sanford、Peter J. H. Scott
DOI:10.1021/acs.orglett.6b02911
日期:2016.10.21
A copper-mediated nucleophilic radiofluorination of aryl- and vinylstannanes with [18F]KF is described. This method is fast, uses commercially available reagents, and is compatible with both electron-rich and electron-deficient arene substrates. This method has been applied to the manual synthesis of a variety of clinically relevant radiotracers including protected [18F]F-phenylalanine and [18F]F-DOPA
描述了用[ 18 F] KF进行的铜介导的芳基和乙烯基锡烷的亲核放射性氟化反应。该方法快速,使用可商购的试剂,并且与富电子和缺电子的芳烃底物兼容。该方法已应用于人工合成各种临床相关的放射性示踪剂,包括受保护的[ 18 F] F-苯丙氨酸和[ 18 F] F-DOPA。另外,已证明[ 18 F] MPPF的自动合成可提供200±20 mCi的临床验证剂量,并具有2400±900 Ci / mmol的高比活度。