Carbon-11 radiolabeled amines constitute a very important class of radioligands that are widely used for positron emission tomography (PET) imaging. Radiolabeling of amines is often achieved through radiomethylation u...Carbon-11 radiolabeled amines constitute a very important class of radioligands that are widely used for positron emission tomography (PET) imaging. Radiolabeling of amines is often achieved through radiomethylation using [11C]CH3I or [11C]CH3OTf under basic conditions in a strictly anhydrous environment. Functional groups such as hydroxyl and carboxyl groups that are often present in the molecules are normally base sensitive and require protection and deprotection, which substantially prolongs and complicates the radiolabeling process. Here we report a versatile approach to a series of C-11 radiolabeled amines prepared through reductive amination using [11C]formaldehyde. Using a variety of substrates bearing different functional groups, we demonstrate the general utility of this method. In contrast to conventional radiomethylation methods, the reductive amination using [11C]formaldehyde can be carried out in an aqueous environment relatively quickly without the need of protection of base-sensitive functional groups.展开更多
背景与目的:11C-乙酸盐因不经泌尿系统排泄而能弥补18F-FDG探测膀胱及周围癌症中的缺陷,但关于其在诊断前列腺癌复发准确性上文献报道不一。本文汇总分析了11C-乙酸盐-PET诊断复发性前列腺癌文献,评价其诊断效能。方法:检索2010年4月前S...背景与目的:11C-乙酸盐因不经泌尿系统排泄而能弥补18F-FDG探测膀胱及周围癌症中的缺陷,但关于其在诊断前列腺癌复发准确性上文献报道不一。本文汇总分析了11C-乙酸盐-PET诊断复发性前列腺癌文献,评价其诊断效能。方法:检索2010年4月前Scifinder、EMBASE和中国期刊全文数据库(CNKI)公开发表的有关11C-乙酸盐-PET诊断复发性前列腺癌的所有文献,对纳入的研究进行方法学质量评价和异质性检验,并用统计软件计算综合特异度和诊断优势比,并绘制综合受试者工作特征曲线(summary receiver operating characteristic,SROC)。结果:共纳入5篇文献,综合灵敏度和特异度分别为83.0%(95%CI=70.2%～91.9%)和70.4%(95%CI=49.8%～86.2%),综合DOR为11.5(95%CI=3.9～34.0)。SROC曲线面积(area under the SROC curve,AUC)为0.84,Q*值为0.77。结论:11C-乙酸盐-PET对于复发性前列腺癌的诊断有较高的价值。展开更多
文摘Carbon-11 radiolabeled amines constitute a very important class of radioligands that are widely used for positron emission tomography (PET) imaging. Radiolabeling of amines is often achieved through radiomethylation using [11C]CH3I or [11C]CH3OTf under basic conditions in a strictly anhydrous environment. Functional groups such as hydroxyl and carboxyl groups that are often present in the molecules are normally base sensitive and require protection and deprotection, which substantially prolongs and complicates the radiolabeling process. Here we report a versatile approach to a series of C-11 radiolabeled amines prepared through reductive amination using [11C]formaldehyde. Using a variety of substrates bearing different functional groups, we demonstrate the general utility of this method. In contrast to conventional radiomethylation methods, the reductive amination using [11C]formaldehyde can be carried out in an aqueous environment relatively quickly without the need of protection of base-sensitive functional groups.
文摘背景与目的:11C-乙酸盐因不经泌尿系统排泄而能弥补18F-FDG探测膀胱及周围癌症中的缺陷,但关于其在诊断前列腺癌复发准确性上文献报道不一。本文汇总分析了11C-乙酸盐-PET诊断复发性前列腺癌文献,评价其诊断效能。方法:检索2010年4月前Scifinder、EMBASE和中国期刊全文数据库(CNKI)公开发表的有关11C-乙酸盐-PET诊断复发性前列腺癌的所有文献,对纳入的研究进行方法学质量评价和异质性检验,并用统计软件计算综合特异度和诊断优势比,并绘制综合受试者工作特征曲线(summary receiver operating characteristic,SROC)。结果:共纳入5篇文献,综合灵敏度和特异度分别为83.0%(95%CI=70.2%～91.9%)和70.4%(95%CI=49.8%～86.2%),综合DOR为11.5(95%CI=3.9～34.0)。SROC曲线面积(area under the SROC curve,AUC)为0.84,Q*值为0.77。结论:11C-乙酸盐-PET对于复发性前列腺癌的诊断有较高的价值。
