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

Radiosynthesis of a carbon-11 labeled PDE5 inhibitor [11C]TPN171 as a new potential PET heart imaging agent. Appl Radiat Isot. 2020 Aug;162:109190 Authors: Xu Z, Jia L, Liu W, Li W, Song Y, Zheng QH 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. PMID: 32501230 [PubMed - as supplied by publisher]
Source: Applied Radiation and Isotopes - Category: Radiology Authors: Tags: Appl Radiat Isot Source Type: research