AN EFFICIENT RADIOSYNTHESIS OF [F-18] FLUOROMISONIDAZOLE

被引:98
作者
LIM, JL
BERRIDGE, MS
机构
[1] CASE WESTERN RESERVE UNIV,DEPT CHEM,CLEVELAND,OH 44106
[2] UNIV HOSP CLEVELAND,CLEVELAND,OH 44106
关键词
D O I
10.1016/0969-8043(93)90110-V
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
An efficient preparation of the hypoxic cell tracer [F-18]3-fluoro-1-(2'-nitro-1'-imidazolyl)-2-propanol ([F-18]fluoromisonidazole) is reported. This radiopharmaceutical is of interest to probe hypoxic tissue in infarcts and tumors. One-step radiolabeling and rapid protection group removal provided 55-80% yield in 50 min. The process is similar to common fluorine labeling procedures, simplifying the procedure for most laboratories, and offers an improvement over more difficult previous methods. The labeling precursor was prepared in five steps from readily available materials in a straightforward reaction scheme.
引用
收藏
页码:1085 / 1091
页数:7
相关论文
共 24 条
[1]   POTENTIAL RADIOSENSITIZING AGENTS - DINITROIMIDAZOLES [J].
AGRAWAL, KC ;
BEARS, KB ;
SEHGAL, RK ;
BROWN, JN ;
RIST, PE ;
RUPP, WD .
JOURNAL OF MEDICINAL CHEMISTRY, 1979, 22 (05) :583-586
[2]  
BAGGETT N, 1960, J CHEM SOC, P2575
[3]  
BEAMAN AG, 1966, ANTIMICROB AGENTS CH, P469
[4]   CYCLIC SULFATES - USEFUL SUBSTRATES FOR SELECTIVE NUCLEOPHILIC-SUBSTITUTION [J].
BERRIDGE, MS ;
FRANCESCHINI, MP ;
ROSENFELD, E ;
TEWSON, TJ .
JOURNAL OF ORGANIC CHEMISTRY, 1990, 55 (04) :1211-1217
[5]  
CHALY T, 1990, APPL RADIAT ISOTOPES, V41, P29
[6]   MISONIDAZOLE AND OTHER HYPOXIA MARKERS - METABOLISM AND APPLICATIONS [J].
FRANKO, AJ .
INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS, 1986, 12 (07) :1195-1202
[7]   VICINAL DIOL CYCLIC SULFATES - LIKE EPOXIDES ONLY MORE REACTIVE [J].
GAO, Y ;
SHARPLESS, KB .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1988, 110 (22) :7538-7539
[8]  
GRIERSON JR, 1989, J NUCL MED, V30, P343
[9]  
GRUNBAUM Z, 1987, J NUCL MED, V28, P68
[10]  
HAMACHER K, 1986, J NUCL MED, V27, P235