发明名称 |
Rapid synthesis and use of 18F-fluoromisonidazole and analogs |
摘要 |
The present invention involves a rapid synthesis of 18F-FMISO and analogs thereof. New precursors such as 1-(2'-nitro-1'-imidazolyl)-2-0-acetyl-3-0-tosylpropanol, glycerol-1,3-ditosylate-2-0-acetylate, 1-(2'-nitro-1'-imidazolyl)-2,3-0-diacetyl-4-0-tosylbutanol and threitol 1,4-di-tosylate-2,3-0-diacetylate, are also important aspects of the invention. A further aspect of the invention is the development of a hydrophilic PET ligand to image tumor hypoxia. Erythrotosyl analogue of 2-nitroimidazone (Ts-ETNIM) was prepared from a mixture of 2-nitromidazole, ditosylthreitol and cesium carbonate at 60 DEG C. for 1 hr. Ts-ETNIM was isolated at 70% yield. [18F]fluoroerythronitroimidazole (FETNIM) was then prepared from Ts-ETNIM and K18F/kryptofix TM . The yield for [18F]FETNIM was 26-30% (60 min, decay corrected). Results of biodistribution and PET studies indicate that [18F]FETNIM has the potential to detect tumor hypoxia and is indicated to be less neurotoxic.
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申请公布号 |
US5886190(A) |
申请公布日期 |
1999.03.23 |
申请号 |
US19970979051 |
申请日期 |
1997.11.26 |
申请人 |
WALLACE, SIDNEY;YANG, DAVID J.;CHERIF, ABDALLAH |
发明人 |
WALLACE, SIDNEY;YANG, DAVID J.;CHERIF, ABDALLAH |
分类号 |
A61K51/04;C07B59/00;C07D233/91;C07D405/06;(IPC1-7):C07D233/91 |
主分类号 |
A61K51/04 |
代理机构 |
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地址 |
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