|
KMID : 1145520200060020011
|
|
Journal of Radiopharmaceuticals and Molecular Probes
2020 Volume.6 No. 2 p.11 ~ p.16
|
|
|
The rapid synthetic strategy of [11C]PIB via disposable column cartridge purification
|
|
Lee Ji-Hye
Li Yansheng
Lee Sang-Yoon
Ido Tatsuo
|
|
|
Abstract
|
|
|
|
PIB is the first amyloid plaque PET image tracer reported for the first time in 2003, and is considered to be the best and is still being utilized due to its very high uptake and kinetic properties. Initially, it was synthesized by radioisotope labeling using a precursor containing a methoxy methyl protection group, but now it is synthesized using a 6-OH precursor that can be easily synthesized in one step using [11C]methyl triflate. Carbon-11 has several limitations in clinical studies using PET because its half-life is as short as 20 minutes. In this study, in order to overcome the difficulty of this half-life, a rapid method using Sep-Pak was adopted instead of HPLC purification to significantly reduce the burden of the purification process and attempted synthesis. As a result, the synthesis time was shortened by more than 50%, and the yield of the final compound was higher than the previous result and showed relatively high specific radioactivity, confirming that it is a strategic method with high applicability for various precursors having primary amines.
|
|
|
KEYWORD
|
|
|
[11C]PIB, Radiochemical yield, [11C]Methylation, tC18 Sep-Pak cartridge
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|