Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease
dc.contributor.author | Dong, Fugui | |
dc.contributor.author | Du, Jie | |
dc.contributor.author | Miao, Caihong | |
dc.contributor.author | Jia, Limeng | |
dc.contributor.author | Li, Wei | |
dc.contributor.author | Wang, Min | |
dc.contributor.author | Zheng, Qi-Huang | |
dc.contributor.author | Xu, Zhidong | |
dc.contributor.department | Radiology and Imaging Sciences, School of Medicine | en_US |
dc.date.accessioned | 2019-12-30T20:15:03Z | |
dc.date.available | 2019-12-30T20:15:03Z | |
dc.date.issued | 2019-12 | |
dc.description.abstract | To develop PET tracers for imaging of Alzheimer's disease, new carbon-11 labeled potent and selective PDE5 inhibitors have been synthesized. The reference standards (5) and (12), and their corresponding desmethylated precursors (6) and (13) were synthesized from methyl 2-amino-5-bromobenzoate and (4-methoxyphenyl)methanamine in multiple steps with 2%, 1%, 1% and 0.2% overall chemical yield, respectively. The radiotracers ([11C]5) and ([11C]12) were prepared from their corresponding precursors 6 and 13 with [11C]CH3OTf through O–11C-methylation and isolated by HPLC combined with SPE in 40–50% radiochemical yield, based on [11C]CO2 and decay corrected to EOB. The radiochemical purity was >99%, and the molar activity (Am) at EOB was in a range of 370–740 GBq/μmol. | en_US |
dc.eprint.version | Author's manuscript | en_US |
dc.identifier.citation | Dong, F., Du, J., Miao, C., Jia, L., Li, W., Wang, M., … Xu, Z. (2019). Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer’s disease. Applied Radiation and Isotopes, 154, 108873. https://doi.org/10.1016/j.apradiso.2019.108873 | en_US |
dc.identifier.uri | https://hdl.handle.net/1805/21621 | |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.relation.isversionof | 10.1016/j.apradiso.2019.108873 | en_US |
dc.relation.journal | Applied Radiation and Isotopes | en_US |
dc.rights | Publisher Policy | en_US |
dc.source | Publisher | en_US |
dc.subject | Phosphodiesterase 5 (PDE5) | en_US |
dc.subject | Carbon-11 labeled PDE5 inhibitors | en_US |
dc.subject | radiosynthesis | en_US |
dc.title | Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease | en_US |
dc.type | Article | en_US |