对甲苯磺酸酯修饰的18F标记策略

18F Labeling Strategy: p-Toluenes Modification

核素示踪是新药研发的重要手段之一,具有灵敏度高、特异性好、直观、真实等优点,结合micro PET等影像设备能提供化合物在活体内的吸收、分布、排泄、转移或转化规律等全面、系统的信息,已成为新药研发中不可或缺的新手段。核素标记是核素示踪的基石。^18F具有和H相似的化学性质,可通过取代反应对化合物进行标记,且半衰期良好、显像性能优良,是理想的示踪核素。主要介绍两种取代作为修饰基团的对甲苯磺酸酯以达到^18F标记目的的标记方法,包括直接标记法和间接标记法。

Radionuclide tracing,which is superior in sensitivity and specificity,is an intuitive measurement in new drug research and investigation.Combined with micro PET or other imaging devices,it can provide comprehensive and systematic information about the absorption,distribution,excretion,transfer,and transformation of compounds in vivo,which has been an indispensable method in the research and development of new drugs.Radio labeling is the cornerst one of radionuclide tracing.^18F,an ideal tracer nuclide,which owns similar chemical properties with H,as well as suitable half-life and imaging performance,can label compounds by substitution reaction.This review of -18F labeling mainly focuses on replacing ptoluene sulfonate,which contains the direct and indirect methods.