SYNTHESIS AND RADIOIODINATION OF A NIDO-1,2-CARBORANYL DERIVATIVE OF 2-NITROIMIDAZOLE

被引:26
作者
WILBUR, DS [1 ]
HAMLIN, DK [1 ]
LIVESEY, JC [1 ]
SRIVASTAVA, RR [1 ]
LARAMORE, GE [1 ]
GRIFFIN, TW [1 ]
机构
[1] UNIV WASHINGTON,DEPT RADIAT ONCOL,SEATTLE,WA 98195
来源
NUCLEAR MEDICINE AND BIOLOGY | 1994年 / 21卷 / 04期
关键词
D O I
10.1016/0969-8051(94)90025-6
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
The synthesis of a nido-carboranyl congener of misonidazole, 1-(3'-nido-carboranyl-2'-hydroxy)propyl-2-nitroimidazole, has been carried out. Alternative methods of preparations were conducted to optimize the chemical yield, with a five step synthesis giving an overall yield (from 1,2-carborane) of 36%. A diastereomeric pair of nido-carboranyl compounds was obtained. The diastereomeric nido-carboranyl misonidazole congeners were (radio)iodinated to yield (> 90%) a mixture of diastereomeric compounds in which the iodine had bonded to a boron atom on the nido-carborane moiety. These compounds will be investigated for their application to boron neutron capture therapy (BNCT) and hypoxia imaging of cancer.
引用
收藏
页码:601 / 611
页数:11
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