Synthesis of a phenolic precursor and its efficient O-[18F]fluoroethylation with purified no-carrier-added [18F]2-fluoroethyl brosylate as the labeling agent.
Synthesis of a phenolic precursor and its efficient O-[18F]fluoroethylation with purified no-carrier-added [18F]2-fluoroethyl brosylate as the labeling agent.
复制标题
酚类前体的合成及其以纯化的无载体添加的[18F]2-氟乙基溴磺酸盐作为标记剂的有效O-[18F]氟乙基化。
DOI：
10.1002/jlcr.3046
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发表时间：
2013
影响因子：
1.8
通讯作者：
Goodman,MarkM
中科院分区：
文献类型：
--
作者：
Jarkas,Nashwa;Voll,RonaldJ;Goodman,MarkM
[18F]2-氟乙基对甲苯磺酸盐也称为[18F]2-氟乙基甲苯磺酸盐，已广泛用于标记正电子发射断层扫描（PET）的放射性配体。 [18F]2-氟乙基-4-溴苯磺酸盐，也称为[18F]2-氟乙基对溴苯磺酸盐([18F]F(CH2)2OBs)，被用作替代放射性标记剂，通过对酚类前体进行O-氟乙基化来制备[18F]FEOHOMADAM，一种HOMADAM的氟乙氧基衍生物。通过反相HPLC纯化，获得未添加载体的[18F]F(CH2)2OBs，平均放射化学产率(RCY)为35%。纯化并干燥的[ 18 F]F(CH 2 ) 2 OBs与酚类前体通过在DMF中加热进行反应，并在HPLC纯化后成功生成[ 18 F]FEOHOMADAM，RCY为21%。版权所有 © 2013 约翰·威利父子有限公司
[18F]2‐Fluoroethyl‐p‐toluenesulfonate also called [18F]2‐fluoroethyl tosylate has been widely used for labeling radioligands for positron emission tomography (PET). [18F]2‐Fluoroethyl‐4‐bromobenzenesulfonate, also called [18F]2‐fluoroethyl brosylate ([18F]F(CH2)2OBs), was used as an alternative radiolabeling agent to prepare [18F]FEOHOMADAM, a fluoroethoxy derivative of HOMADAM, byO‐fluoroethylating the phenolic precursor. Purified by reverse‐phase HPLC, the no‐carrier‐added [18F]F(CH2)2OBs was obtained in an average radiochemical yield (RCY) of 35%. The reaction of the purified and dried [18F]F(CH2)2OBs with the phenolic precursor was performed by heating in DMF and successfully produced [18F]FEOHOMADAM, after HPLC purification, in RCY of 21%. Copyright © 2013 John Wiley & Sons, Ltd.