Radiosynthesis of a carbon-11 labeled tetrahydrobenzisoxazole derivative as a new PET probe for γ-secretase imaging in Alzheimer's disease
dc.contributor.author | Xu, Zhidong | |
dc.contributor.author | Miao, Caihong | |
dc.contributor.author | Dong, Fugui | |
dc.contributor.author | Jia, Limeng | |
dc.contributor.author | Li, Wei | |
dc.contributor.author | Wang, Min | |
dc.contributor.author | Liu, Wenqing | |
dc.contributor.author | Zheng, Qi-Huang | |
dc.contributor.department | Radiology and Imaging Sciences, School of Medicine | en_US |
dc.date.accessioned | 2021-10-06T19:07:08Z | |
dc.date.available | 2021-10-06T19:07:08Z | |
dc.date.issued | 2020-01 | |
dc.description.abstract | 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 [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. | en_US |
dc.eprint.version | Author's manuscript | en_US |
dc.identifier.citation | Xu, 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.2019.108915 | en_US |
dc.identifier.uri | https://hdl.handle.net/1805/26697 | |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.relation.isversionof | 10.1016/j.apradiso.2019.108915 | en_US |
dc.relation.journal | Applied Radiation and Isotopes | en_US |
dc.rights | Publisher Policy | en_US |
dc.source | Author | en_US |
dc.subject | γ-Secretase | en_US |
dc.subject | Carbon-11 labeled γ-secretase modulator (GSM) | en_US |
dc.subject | radiosynthesis | en_US |
dc.title | Radiosynthesis of a carbon-11 labeled tetrahydrobenzisoxazole derivative as a new PET probe for γ-secretase imaging in Alzheimer's disease | en_US |
dc.type | Article | en_US |