An improved total synthesis of PET HSV-tk gene expression imaging agent 9-[(3-[18F]fluoro-1-hydroxy-2-propoxy)methyl]guanine ([18F]FHPG)

被引:9
作者
Wang, JQ
Zheng, QH
Fei, XS
Liu, X
Gardner, TA
Kao, CH
Raikwar, SP
Glick-Wilson, BE
Sullivan, ML
Mock, BH
Hutchins, GD
机构
[1] Indiana Univ, Sch Med, Dept Radiol, Indianapolis, IN 46202 USA
[2] Indiana Univ, Sch Med, Dept Urol, Indianapolis, IN 46202 USA
关键词
9-[(3-[F-18]fluoro-1-hydroxy-2-propoxy)methyl]guanine ([F-18]FHPG); ganciclovir (GCV); synthesis; positron emission tomography (PET); herpes simplex virus thymidine kinase (HSV-tk); gene expression;
D O I
10.1081/SCC-120028365
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
An improved total synthesis of [F-18]FHPG starting from 1,3-dibenzyloxy2-propanol and guanine has been developed. [F-18]FHPG was prepared by nucleophilic substitution of the appropriate precursor with [F-18]KF/ Kryptofix 2.2.2 followed by a quick deprotection reaction and purification with a simplified Silica Sep-Pak solid-phase extraction (SPE) method in 10-15% radiochemical yield, and 70 min synthesis time from end of bombardment (EOB).
引用
收藏
页码:917 / 932
页数:16
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