发明名称 |
RAPID SYNTHESIS AND USE OF <18>F-FLUOROMISONIDAZOLE AND ANALOGS |
摘要 |
The present invention involves a rapid synthesis of <18> F-FMISO and analogs thereof. New precursors such as 1-(2'-nitro-1'-imidazolyl)-2-O-acetyl-3-O-tosylpropanol, glycerol-1,3-ditosylate-2-O-acetylate, 1-(2'-nitro-1'-imidazolyl)-2,3-O-diacetyl-4-O-tosylbutanol and threitol 1,4-di-tosylate-2,3-O-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. [<18>F]fluoroerythronitroimidazole (FETNIM) was then prepared from Ts-ETNIM and K<18>F/kryptofix3. The yield for [<18>F]FETNIM was 26-30 % (60 min, decay corrected). Results of biodistribution and PET studies indicate that [<18>F]FETNIM has the potential to detect tumor hypoxia and is indicated to be less neurotoxic. |
申请公布号 |
WO9509844(A1) |
申请公布日期 |
1995.04.13 |
申请号 |
WO1994US11246 |
申请日期 |
1994.10.04 |
申请人 |
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM;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 |
主分类号 |
A61K51/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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