肿瘤显像剂O-(^(18)F-氟代正烷基)-L-酪氨酸的合成  

Synthesis of O-(^(18)F-fluoroalkyl)-L-tyrosine as tumor imaging agents

作　　者：唐刚华[1] 唐小兰[2] 罗磊[1] 

机构地区：[1]第一军医大学南方医院南方PET中心,广州510515 [2]华南农业大学理学院,广州510642

出　　处：《核技术》2003年第8期619-622,共4页Nuclear Techniques

摘　　要：O-(2-18F-氟代乙基)-L-酪氨酸(FET)和O-(3-18F-氟代丙基)-L-酪氨酸(FPT)由两步法制备。18F-分别与二对甲苯磺酸乙二酯(TsOCH2CH2OTs)和二对甲苯磺酸丙二酯(TsOCH2CH2CH2OTs)发生亲核取代反应,生成对甲苯磺酸-2-18F-氟代乙酯(18F CH2CH2OTs)和对甲苯磺酸-3-18F-氟代丙酯(18FCH2CH2CH2OTs),后两者再分别与L-酪氨酸二钠反应生成FET和FPT,总反应时间小于90 min。终产物FET和FPT用乙腈沉淀法分离纯化,未校正总放化产率分别为4.7%和8%。用HPLC法分离纯化,未校正总放化产率分别为20%和30%。FET和FPT注射液放化纯度大于95%,各质量控制指标符合放射性药物质量要求。O-(2-18F-Fluoroethyl)-L-tyrosine (FET) and O-(3-18F-fluoropropyl)-L-tyrosine (FPT) were prepared by a two-step reaction. First, nucleophilic fluorination reaction of 18F-fluoride with 1,2-di (4-methylphenylsulfonyloxy) ethane (TsOCH2CH2OTs) and 1,3-di(4-methylphenylsulfonyloxy) propane (TsOCH2CH2CH2OTs) gave 2-18F-1-(4- methylphenylsulfonyloxy) ethane (18FCH2CH2OTs) and 3-18F-1-(4-methylphenylsulfonyloxy) propane (18FCH2CH2CH2 OTs), respectively. Then, 18F-fluoroalkylation of L-tyrosine di-sodium salt formed FET and FPT respectively, with the whole synthesis time of less than 90 min. Purification of resultant FET and FPT by acetonitrile precipitation gave an overall radiochemical yield of 4.7% and 8% with no decay correction, and purification by HPLC gave an overall radiochemical yield of 20% and 30% with no decay correction, respectively. The radiochemical purity of FET and FPT injection was above 95%, and all quality parameters met the quality requirements of radiopharmaceuticals.

关 键 词：O-(2-^18F-氟代乙基)-L-酪氨酸 O-(3-^18F-氟代丙基)-L-酪氨酸 合成 质量控制 

分 类 号：R817.4[医药卫生—影像医学与核医学]