作者:Mads H. Rønnest、Felix Nissen、Palle J. Pedersen、Thomas O. Larsen、Walter Mier、Mads H. Clausen
DOI:10.1002/ejoc.201300419
日期:2013.7
A novel technique to label ortho-, meta-, and para-trimethylsilyl-substituted aryl substituents with radioactive iodide is described. The method takes advantage of the ipso-directing and activating properties of trimethylsilyl substituents on the arenes. The method was demonstrated on a griseofulvin analogue with promising anticancer properties and on lidocaine, a widely used local anesthetic drug
描述了一种用放射性碘标记邻、间和对三甲基甲硅烷基取代的芳基取代基的新技术。该方法利用芳烃上三甲基甲硅烷基取代基的同向导向和活化特性。该方法在具有良好抗癌特性的灰黄霉素类似物和广泛使用的局部麻醉药物利多卡因上得到了证明。在所有情况下,用 Tl(OCOCF3)3 和 Na125I 处理三甲基甲硅烷基前体始终提供超过 95% 的放射性纯度。