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 (A_m) at EOB was in a range of 370–740 GBq/μmol.

为了开发用于心脏病成像的PET示踪剂，已经合成了一种新的碳11标记的强效选择性PDE5抑制剂[ ¹¹ C] TPN171（[ ¹¹ C] 9）。参考标准TPN171（9）及其相应的前体desmethyl-TPN171（11）由3-氧戊酸甲酯和2-羟基苄腈分9步和10步合成，总化学收率分别为31％和25％。放射性示踪剂[ ¹¹ C] TPN171由具有[ ¹¹ C] CH ₃ OTf的脱甲基-TPN171通过N - ¹¹制备C-甲基化并通过HPLC纯化分离，然后通过SPE配制，基于[ ¹¹ C] CO _2的放射化学产率为45-55％，并将衰变校正为EOB。放射化学纯度> 99％，在EOB的摩尔活度（A _m）为370–740 GBq /μmol。