摘要
目的探索tau蛋白正电子核素探针[^(18)F]MK-6240标记前体的合成工艺。方法以3-氯异喹啉为起始原料,通过硝化、还原、缩合、硝化、亲核取代、水解等反应路径,成功制备了[^(18) F]MK-6240标记前体,结构用氢谱和质谱鉴定。结果以7步直线式合成反应,约6.4%的总收率制备了[^(18) F]MK-6240标记前体。结论所用方法原料便宜易得,且合成步骤简单,大大提高了收率,适合[^(18)F]MK-6240标记前体的实验室制备。
OBJECTIVE To investigate the synthesis of the radio-labeling precursor of a novel tau protein PET tracer[^(18)F]MK-6240.METHODS The target compound was successfully synthesized from 3-chloroisoquinoline via nitrification,reduction,nucleophilic substitution,and hydrolysis reactions.RESULTS With overall 6.4%isolated yield,the radio-labeling precursor of[^(18)F]MK6240 was successfully prepared under laboratory conditions and characterized by 1HNMR and mass spectrum.CONCLUSION Based on the commercially available low-cost starting material and convenient reaction conditions,a novel and highly efficient synthesis route is developed and may be applied in clinical for the production of[^(18)F]MK-6240.
作者
蔡玥
潘立立
吴小艾
CAI Yue;PAN Lili;WU Xiaoai(Department of Science and Technology,West China Hospital,Sichuan University,Chengdu,Sichuan,610041 P.R.China;Department of Nuclear Medicine,West China Hospital,Sichuan University,Chengdu,Sichuan,610041 P.R.China)
出处
《华西药学杂志》
CAS
CSCD
2022年第3期229-232,共4页
West China Journal of Pharmaceutical Sciences
基金
四川省科技厅重点项目(编号:2017JY0324)。
