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作 者:殷正旭 徐国强 陈腾祥[1,2] 韩俊斌 Yin Zhengxu;Xu Guoqiang;Chen Tengxiang;Han Junbin(School of Basic Medical Sciences,Guizhou Medical University,Guiyang 561113;Transformation Engineering Research Center of Chronic Disease Diagnosis and Treatment,Guizhou Medical University,Guiyang 561113)
机构地区:[1]贵州医科大学基础医学院,贵阳561113 [2]贵州医科大学慢性病诊疗改造工程研究中心,贵阳561113
出 处:《化学学报》2024年第11期1120-1123,共4页Acta Chimica Sinica
基 金:国家自然科学基金(Nos.22078161,22108124)资助。
摘 要:氟胺是生物活性分子中一类重要的结构,其^(18)F放射标记方法研究将促进β-氟胺类分子的活体可视化评估与研究.在此次研究中,引入新型[^(18)F]AgF标记试剂以促进氮杂环丙烷氟化开环反应以制备了[^(18)F]β-氟胺类衍生物.前期条件优化结果显示标记反应不需要添加额外银盐和酸,且反应对空气和微量的水有着良好的兼容性,避免了繁杂的放射性除水过程.高效液相色谱分离谱图显示标记产物放射化学转化率大于80%,进一步对收集后的放射产物分析显示其放射收率大部分在30%以上,关键标记产物2a比活度为15.6±2.9 GBq/μmol.随后底物适用性筛选也表明反应对于环状融合和脂肪烃等多样的氮杂环丙烷都有着较为良好的兼容性.总之,该研究发展了一种针对β-氟胺较为通用的^(18)F放射标记方法,反应简单高效,为β-氟胺类的相关分子可视化研究提供了新的思路.Fluoroamines represent a crucial motif in biological and pharmaceutical sciences,largely due to the introduction of fluorine,which enhances the binding affinity,metabolic stability,and bioavailability of target molecules.This makes them highly valuable in the realm of drug discovery.Among the various radionuclides utilized in nuclear medicine imaging,fluorine-18(^(18)F)is the most prevalent.Its favorable physicochemical properties,including a half-life of 109.8 min,facilitate optimal target-to-background ratios in imaging processes.Additionally,^(18)F is advantageous for multi-step synthesis and transportation,and its decay produces oxygen-18(^(18)O)atoms,which are harmless to humans.Given this context,our research aims to synthesizeβ-fluoroamine positron emission computed tomography(PET/CT)imaging agents with significant potential applications.Developing an effective radiolabeling methodology will greatly advance the in vivo visualization and evaluation of target molecules.In this study,we employed[^(18)F]AgF in the hydro fluorination of aziridines to achieve the radiosynthesis of[^(18)F]β-fluoroamines.Preliminary optimizations revealed that additional silver salts and acids were unnecessary,and the labeling process does not require azeotropic drying.This method exhibits good compatibility with light,water,and oxygen,successfully circumventing the complex radioactive dehydration processes while also facilitating automatic labeling.Moreover,the reaction delivered excellent radiochemical conversion(RCC)and moderate radiochemical yield(RCY)in optimized conditions.Radioactive high performance liquid chromatography(Radio-HPLC)spectrum shows that the radiochemical conversion rate of labeled products is more than 80%.Further analysis of the collected radioactive products shows that most of the reactions have a radiation yield of more than 30%.For the key molecule 2a,we conducted a calculation of the specific activity.The higher the specific activity,the greater its potential for biological applications.After three ex
关 键 词:放射性氟化反应 β-氟胺 正电子发射计算机断层扫描 开环反应
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