【摘要】 目的制备前列腺癌显像剂¹⁸F-8-乙氧基-2-（4-氟苯基）-3-硝基-2H-色烯的前体8-乙氧基-2-（4-N,N,N-三甲基氨基苯基）-3-硝基-2H-色烯季胺三氟甲磺酸盐;用前体和放射性核素¹⁸F合成¹⁸F-8-乙氧基-2-（4-氟苯基）-3-硝基-2H-色烯。方法以2-羟基-1-乙氧基-3-醛基苯为起始原料,经烯化、环化、磺化、成盐反应得到标记前体8-乙氧基-2-（4-N,N,N-三甲基氨基苯基）-3-硝基-2H-色烯季胺三氟甲磺酸盐;然后与放射性核素¹⁸F经亲核氟代反应,得到¹⁸F-8-乙氧基-2-（4-氟苯基）-3-硝基-2H-色烯。标记前体8-乙氧基-2-（4-N,N,N-三甲基氨基苯基）-3-硝基-2H-色烯季胺三氟甲磺酸盐及各步反应中间体的结构均经核磁共振谱和质谱确证。结果与结论成功合成前列腺癌诊断显影剂¹⁸F-8-乙氧基-2-（4-氟苯基）-3-硝基-2H-色烯,标记率为（25.8±2.6）%（n=5,未经衰减校正）,TLC测定其放化纯度（RCP）为97.5%,为进一步临床研究奠定了基础。更多还原

【Abstract】 ¹⁸F-8-ethoxy-2-（4-fluorophenyl）-3-nitro-2H-chromene precursor was synthesized from 2-hydroxy-1-ethoxyl-3-aldehyde benzene via olefination alkylene,cyclization,sulfonation,salt formation,etc.Synthesis of ¹⁸F-8-ethoxy-2-（4-fluorophenyl）-3-nitro-2H-chromene was through nucleophilic substitution by using fluorine multi-function synthesis module.The chemical structures of the precursor 8-ethoxylated-2-（4-N,N,N-trimethylaminophenyl）-3-nitro-2H-chromene tetramine trifluoromethylsulfonate and all intermediates were verified by ¹H-NMR,¹³C-NMR and LC-MS.¹⁸F-8-ethoxy-2-（4-fluorophenyl）-3-nitro-2H-chromene was obtained a radiochemical yield of（25.8±2.6）%（n=5,nodecay corrected） in a total synthesis time of about 40 min and radiochemical purity of >97% determined by TLC.It lays a foundation for further clinical research.更多还原