一种用于阿尔茨海默病中γ-分泌酶成像的新型正电子发射断层显像（PET）探针——碳-11标记的四氢苯并异恶唑衍生物的放射性合成。
Radiosynthesis of a carbon-11 labeled tetrahydrobenzisoxazole derivative as a new PET probe for γ-secretase imaging in Alzheimer's disease.
作者信息
Xu Zhidong, Miao Caihong, Dong Fugui, Jia Limeng, Li Wei, Wang Min, Liu Wenqing, Zheng Qi-Huang
机构信息
College of Chemical & Pharmaceutical Engineering, Key Laboratory of Molecular Chemistry for Medicine of Hebei Province, Hebei University of Science & Technology, Shijiazhuang, Hebei, 050018, China; Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, College of Chemistry and Environmental Science, Hebei University, Baoding, Hebei, 071002, China.
Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, College of Chemistry and Environmental Science, Hebei University, Baoding, Hebei, 071002, China.
出版信息
Appl Radiat Isot. 2020 Jan;155:108915. doi: 10.1016/j.apradiso.2019.108915. Epub 2019 Oct 1.
To develop PET radiotracers for imaging of Alzheimer's disease, a new carbon-11 labeled potent and selective γ-secretase modulator (GSM) has been synthesized. The reference standard tetrahydrobenzisoxazole derivative 8 and its desmethylated precursor 9 were synthesized from cyclohex-2-en-1-one and 3-hydroxy-4-nitrobenzaldehyde in eight and nine steps with 11% and 5% overall chemical yield, respectively. The radiotracer [C]8 was prepared from its corresponding precursor 9 with [C]CHOTf through O-C-methylation and isolated by RP-HPLC combined with SPE in 45-50% radiochemical yield, based on [C]CO and decay corrected to EOB. The radiochemical purity was >99%, and the molar activity (A) at EOB was 555-740 GBq/μmol.
为开发用于阿尔茨海默病成像的正电子发射断层显像（PET）放射性示踪剂，已合成了一种新的碳-11标记的强效且选择性γ-分泌酶调节剂（GSM）。参考标准四氢苯并异恶唑衍生物8及其去甲基化前体9由环己-2-烯-1-酮和3-羟基-4-硝基苯甲醛分别经八步和九步合成，总化学产率分别为11%和5%。放射性示踪剂[C]8由其相应前体9与[C]CHOTf通过O-C-甲基化制备，并通过反相高效液相色谱（RP-HPLC）结合固相萃取（SPE）分离，基于[C]CO并校正至给药结束时（EOB）的衰变，放射化学产率为45 - 50%。放射化学纯度>99%，给药结束时的摩尔活度（A）为555 - 740 GBq/μmol。
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