Department of Oncology, University of Alberta, Edmonton, Canada.
Chem Commun (Camb). 2019 Jan 24;55(9):1310-1313. doi: 10.1039/c8cc08717b.
The first application of sulfo-click chemistry with 18F-labeled thio acids is described. The simple one-pot/three-component reaction proceeded rapidly within 30 min using mild reaction conditions to give various 18F-labeled small molecule N-acylsulfonamides in radiochemical conversions of 38-99%, and radiolabeled peptides in 20-25% isolated and decay-corrected radiochemical yields.
本文首次描述了带有 18F 标记的硫代酸的磺基点击化学的应用。该反应条件温和,简单的一锅三步反应在 30 分钟内迅速进行,得到了各种 18F 标记的小分子 N-酰基磺酰胺,放射化学转化率为 38-99%,放射性标记肽的分离和衰变校正的放射化学产率为 20-25%。