Xu, ZhidongMiao, CaihongDong, FuguiJia, LimengLi, WeiWang, MinLiu, WenqingZheng, Qi-Huang2021-10-062021-10-062020-01Xu, Z., Miao, C., Dong, F., Jia, L., Li, W., Wang, M., Liu, W., & Zheng, Q.-H. (2020). Radiosynthesis of a carbon-11 labeled tetrahydrobenzisoxazole derivative as a new PET probe for γ-secretase imaging in Alzheimer’s disease. Applied Radiation and Isotopes, 155, 108915. https://doi.org/10.1016/j.apradiso.2019.108915https://hdl.handle.net/1805/26697To 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 [11C]8 was prepared from its corresponding precursor 9 with [11C]CH3OTf through O–11C-methylation and isolated by RP-HPLC combined with SPE in 45–50% radiochemical yield, based on [11C]CO2 and decay corrected to EOB. The radiochemical purity was >99%, and the molar activity (Am) at EOB was 555–740 GBq/μmol.enPublisher Policyγ-SecretaseCarbon-11 labeled γ-secretase modulator (GSM)radiosynthesisArticle