Radiosynthesis of a carbon-11 labeled PDE5 inhibitor [11C]TPN171 as a new potential PET heart imaging agent

Zhidong Xu, Limeng Jia, Wenqing Liu, Wei Li, Ying Song, Qi Huang Zheng

Research output: Contribution to journalArticle

Abstract

To develop PET tracers for imaging of heart disease, a new carbon-11 labeled potent and selective PDE5 inhibitor [11C]TPN171 ([11C]9) has been synthesized. The reference standard TPN171 (9) and its corresponding precursor desmethyl-TPN171 (11) were synthesized from methyl 3-oxovalerate and 2-hydroxybenzonitrile in 9 and 10 steps with 31% and 25% overall chemical yield, respectively. The radiotracer [11C]TPN171 was prepared from desmethyl-TPN171 with [11C]CH3OTf through N-11C-methylation and isolated by HPLC purification followed by SPE formulation in 45–55% 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 number109190
JournalApplied Radiation and Isotopes
Volume162
DOIs
StatePublished - Aug 2020

Keywords

  • Carbon-11 labeled PDE5 inhibitor
  • Heart disease
  • Phosphodiesterase 5 (PDE5)
  • Positron emission tomography (PET)
  • Radiosynthesis
  • [C]TPN171

ASJC Scopus subject areas

  • Radiation

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