Haskali Mohammad B, Roselt Peter D, Karas John A, Noonan Wayne, Wichmann Christian W, Katsifis Andrew, Hicks Rodney J, Hutton Craig A
School of Chemistry, The University of Melbourne, Vic., 3010, Australia; Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Vic., 3010, Australia; The Centre for Molecular Imaging and Translational Research Laboratory, The Peter MacCallum Cancer Centre, Melbourne, Vic., Australia.
J Labelled Comp Radiopharm. 2013 Dec;56(14):726-30. doi: 10.1002/jlcr.3111. Epub 2013 Sep 16.
The versatile (18) F-labeled prosthetic group, 4-nitrophenyl 2-[(18) F]fluoropropionate ([(18) F]NFP), was synthesized in a single step in 45 min from 4-nitrophenyl 2-bromopropionate, with a decay corrected radiochemical yield of 26.2% ± 2.2%. Employing this improved synthesis of [(18) F]NFP, [(18) F]GalactoRGD - the current 'gold standard' tracer for imaging the expression of αV β3 integrin - was prepared with high specific activity in 90 min and 20% decay corrected radiochemical yield from [(18) F]fluoride.
多功能的(18)F标记的 Prosthetic 基团,4-硝基苯基2-[(18)F]氟丙酸酯([(18)F]NFP),由4-硝基苯基2-溴丙酸酯在一步反应中于45分钟内合成,衰变校正后的放射化学产率为26.2%±2.2%。采用这种改进的[(18)F]NFP合成方法,以高比活度在90分钟内由[(18)F]氟化物制备出[(18)F]半乳糖RGD——目前用于成像αVβ3整合素表达的“金标准”示踪剂,衰变校正后的放射化学产率为20%。