Synthesis of 8-[18F]fluoroguanine derivatives:: In vivo probes for imaging gene expression with positron emission tomography

被引：57

作者：

Namavari, M

Barrio, JR

Toyokuni, T

Gambhir, SS

Cherry, SR

Herschman, HR

Phelps, ME

Satyamurthy, N ^{[1
]}

机构：

[1] Univ Calif Los Angeles, Sch Med, Dept Mol & Med Pharmacol, Div Nucl Med, Los Angeles, CA 90095 USA

[2] Univ Calif Los Angeles, DOE, Lab Struct Biol & Mol Med, Los Angeles, CA 90024 USA

[3] Univ Calif Los Angeles, Sch Med, Inst Mol Biol, Los Angeles, CA 90024 USA

[4] Univ Calif Los Angeles, Sch Med, Jonsson Comprehens Canc Ctr, Los Angeles, CA 90024 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 02期

关键词：

8-[F-18]fluoroganciclovir; 8-[F-18]fluuropenciclovir; 8-[F-18]fluoroacyclovir; PET; gene expression;

D O I：

10.1016/S0969-8051(99)00095-5

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

A new method for the preparation of 8-[F-18]fluoroguanine derivatives based on a direct radiofluorination reaction has been developed. The radiofluorination of ganciclovir (1a) with [F-18]F-2 was carried out in absolute ethanol in the presence of tetraethylammonium hydroxide at room temperature to give 8-[F-18]fluoroganciclovir (3a) in an approximately 1% radiochemical yield. Similarly, 8-[F-18]fluoropenciclovir (3b), 8-[F-18]fluoroacyclovir (3c), and 8-[F-18]fluoroguanosine (3d) were synthesized from penciclovir (1b), acyclovir (1c), and guanosine (1d), respectively, using [F-18]F-2. The structural analyses of the final products (3a, 3b, 3c, and 3d) were carried out after F-18 decay by H-1, C-13, and F-18 nuclear magnetic resonance and high resolution mass spectroscopy. NUCL MED BIOL 27;2:157-162, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：157 / 162

页数：6

共 29 条

[1] Synthesis and preliminary evaluation of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG):: A new potential imaging agent for viral infection and gene therapy using PET [J].