Radiosynthesis of 2'-deoxy-2'-[18F]-fluoro-5-methyl-1-β-L-arabinofuranosyluracil([18F]-L-FMAU) for PET

被引:16
|
作者
Mukhopadhyay, Uday [1 ]
Pal, Ashutosh [1 ]
Gelovani, Juri G. [1 ]
Bornmann, William [1 ]
Alauddin, Mian M. [1 ]
机构
[1] Univ Texas, MD Anderson Canc Ctr, Dept Expt Diag Imaging, Houston, TX 77030 USA
关键词
fluorine-18; nucleoside; L-FMAU; hepatitis B;
D O I
10.1016/j.apradiso.2007.04.003
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Radiosynthesis of 2'-deoxy-2-[F-18]-fluoro-5-methyl-1-beta-L-arabinofuranosyluracil ([F-18]-L-FMAU) is reported. Compound 1 was synthesized and converted to 2-triflate 2. Compound 3 was prepared from 2 using tetrabutylammonium[F-18]fluoride, converted to 4, and then coupled with 5. The crude product was hydrolyzed, and purified by HPLC to obtain 7a. The radiochemical yield of [F-18]-L-FMAU was 26% decay corrected (d.c.) in four runs with radiochemical purity >99% and specific activity 2200 mCi/mu mol. The synthesis time was 3.3-3.5 h from the end of bombardment (EOB). (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:941 / 946
页数:6
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