Synthesis of new hypoxia markers EF1 and [18F]-EF1

被引：32

作者：

Kachur, AV

Dolbier, WR

Evans, SM

Shiue, CY

Shiue, GG

Skov, KA

Baird, IR

James, BR

Li, AR

Roche, A

Koch, CJ ^{[1
]}

机构：

[1] Univ Penn, Dept Radiat Oncol, Philadelphia, PA 19104 USA

[2] Univ Penn, Sch Med, Dept Radiol, Philadelphia, PA 19104 USA

[3] Univ Penn, Sch Vet Med, Dept Clin Studies, Philadelphia, PA 19104 USA

[4] Univ Florida, Dept Chem, Gainesville, FL 32611 USA

[5] British Columbia Canc Res Ctr, Vancouver, BC V5Z 1L3, Canada

[6] Univ British Columbia, Dept Chem, Vancouver, BC V6T 1Z1, Canada

来源：

APPLIED RADIATION AND ISOTOPES | 1999年 / 51卷 / 06期

基金：

加拿大自然科学与工程研究理事会;

关键词：

D O I：

10.1016/S0969-8043(99)00096-2

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

We report on the preparation of a hypoxia marker 2-(2-nitroimidazol-1[H]-yl)-N-(3-fluoropropyl)acetamide (EF1) and its F-18 analog, 2-(2-nitroimidazol-1[H]-yl)-N-(3-[F-18]fluoropropyl)acetamide ([F-18]-EF1). Two methods for the preparation of 3-fluoropropylamine, the EF1 side chain, are described. [F-18]-EF1 was prepared with a radiochemical yield of 2% by nucleophilic substitution of bromine in 2-(2-nitroimidazol-1[H]-yl)-N-(3-bromopropyl) acetamide (EBrl) by carrier-added F-18 in DMSO at 120 degrees C. Our results demonstrate the preparation of clinically relevant amounts of [F-18]-EF1 for use as a non-invasive hypoxia marker with detection using positron emission tomography (PET). (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：643 / 650

页数：8

共 33 条

[21] RADIOIODINATED 1-(2-FLUORO-4-IODO-2,4-DIDEOXY-BETA-L-XYLOPYRANOSYL)-2-NITROIMIDAZOLE - A NOVEL PROBE FOR THE NONINVASIVE ASSESSMENT OF TUMOR HYPOXIA [J].