Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease

F. Dong, Jie Du, Caihong Miao, Limeng Jia, Wei Li, Min Wang, Qi-Huang Zheng, Zhidong Xu

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Article number108873
JournalApplied Radiation and Isotopes
Volume154
DOIs
StatePublished - Dec 1 2019

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inhibitors
methylation
carbon
tracers
purity
decay

Keywords

  • Alzheimer's disease (AD)
  • Carbon-11 labeled PDE5 inhibitors
  • Phosphodiesterase 5 (PDE5)
  • Positron emission tomography (PET)
  • Radiosynthesis

ASJC Scopus subject areas

  • Radiation

Cite this

Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease. / Dong, F.; Du, Jie; Miao, Caihong; Jia, Limeng; Li, Wei; Wang, Min; Zheng, Qi-Huang; Xu, Zhidong.

In: Applied Radiation and Isotopes, Vol. 154, 108873, 01.12.2019.

Research output: Contribution to journalArticle

Dong, F. ; Du, Jie ; Miao, Caihong ; Jia, Limeng ; Li, Wei ; Wang, Min ; Zheng, Qi-Huang ; Xu, Zhidong. / Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease. In: Applied Radiation and Isotopes. 2019 ; Vol. 154.
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AU - Li, Wei

AU - Wang, Min

AU - Zheng, Qi-Huang

AU - Xu, Zhidong

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KW - Carbon-11 labeled PDE5 inhibitors

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KW - Positron emission tomography (PET)

KW - Radiosynthesis

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