用于正电子发射断层显像（PET）的2'-脱氧-2'-[18F] -氟-5-甲基-1-β-L-阿拉伯呋喃糖基尿嘧啶（[18F] -L-FMAU）的放射性合成。
Radiosynthesis of 2'-deoxy-2'-[18F]-fluoro-5-methyl-1-beta-L-arabinofuranosyluracil ([18F]-L-FMAU) for PET.
作者信息
Mukhopadhyay Uday, Pal Ashutosh, Gelovani Juri G, Bornmann William, Alauddin Mian M
机构信息
Department of Experimental Diagnostic Imaging, University of Texas M D Anderson Cancer Center, Houston, TX, USA.
出版信息
Appl Radiat Isot. 2007 Aug;65(8):941-6. doi: 10.1016/j.apradiso.2007.04.003. Epub 2007 Apr 14.
Radiosynthesis of 2'-deoxy-2'-[(18)F]-fluoro-5-methyl-1-beta-L-arabinofuranosyluracil ([(18)F]-L-FMAU) is reported. Compound 1 was synthesized and converted to 2-triflate 2. Compound 3 was prepared from 2 using tetrabutylammonium[(18)F]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 [(18)F]-L-FMAU was 26% decay corrected (d.c.) in four runs with radiochemical purity >99% and specific activity 2200 mCi/micromol. The synthesis time was 3.3-3.5h from the end of bombardment (EOB).
报道了2'-脱氧-2'-[(18)F]-氟-5-甲基-1-β-L-阿拉伯呋喃糖基尿嘧啶([(18)F]-L-FMAU)的放射性合成。合成了化合物1并将其转化为2-三氟甲磺酸酯2。使用四丁基铵[(18)F]氟化物由2制备化合物3，将其转化为4，然后与5偶联。粗产物水解，并通过高效液相色谱法纯化以获得7a。[(18)F]-L-FMAU的放射化学产率在四次运行中为26%衰变校正(d.c.)，放射化学纯度>99%，比活度为2200 mCi/μmol。从轰击结束(EOB)起合成时间为3.3 - 3.5小时。
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