Synthesis of [11C]uric acid, using [11C]phosgene, as a possible biomarker in PET imaging for diagnosis of gout
作者:Keiji Yashio、Yumiko Katayama、Tadayuki Takashima、Naoki Ishiguro、Hisashi Doi、Masaaki Suzuki、Yasuhiro Wada、Ikumi Tamai、Yasuyoshi Watanabe
DOI:10.1016/j.bmcl.2011.11.055
日期:2012.1
The synthesis and in vivo evaluation of 11C -labeled uric acid ([11C]1), a potential imaging agent for the diagnosis of urate-related life-style diseases, was performed using positron emission tomography (PET) image analysis. First, the synthesis of [11C]1 was achieved by reacting 5,6-diaminouracil (2) with 11C-labeled phosgene ([11C]COCl2). The radiochemical yield of [11C]1 was 37 ± 7% (decay-corrected
使用正电子发射断层扫描(PET)图像分析进行11 C标记的尿酸([ 11 C] 1)的合成和体内评估,尿酸是诊断与尿酸盐有关的生活方式疾病的潜在成像剂。首先,通过使5,6-二氨基尿嘧啶(2)与11 C标记的光气([ 11 C] COCl 2)反应来实现[ 11 C] 1的合成。合成结束时,[ 11 C] 1的放射化学产率为37±7%(基于[ 11 C] COCl 2进行衰减校正),比活度为96–152 GBq /μmol。n = 6)。从轰炸结束,包括制剂制备,平均放射合成时间约为30分钟,放射化学纯度> 98%。其次,在1,8-双(二甲基氨基)萘的存在下,使用带有[ 11 C] COCl 2的5,6-二氨基尿嘧啶硫酸盐(3)优化了[ 11 C] 1的合成方法。[ 11 C] 1通过这种方法合成,放射化学产率为36±6%,比放射性为89–142 GBq /μmol,放射化学纯度为98%(n