Synthesis of N-[4-(2'-[18f]Fluoroalkoxybenzoyl)]- and N-(3-[123i]Iodo-4-methoxybenzoyl)pyrrolidin-2-ones As Potential Brain Imaging Agents
作者:George Kabalka、Murthy R. Akula、David Blevins、Dustin Osborne
DOI:10.3987/com-18-s(t)75
日期:——
The microfluidic synthesis of promising brain imaging PET agents N-[4-(2'-[F-18]fluoroalkyloxybenzoylApyrrolidin-2-ones 13a-c was accomplished by nucleophilic radiofluorination of the corresponding tosylate precursors 9a-c with Kryptofix-potassium carbonate-[F-18] fluoride. Decay corrected radiochemical yields of 35 +/- 5% (13a), 38 +/- 8% (13b) and 40 +/- 15% (13c) were obtained with radiochemical purities of >= 93%. The total reaction time, including HPLC purification was 40 min. N-(3-[I-123]Iodo-4-methoxybenzoyl)pyrrolidin-2-one, 18, was prepared by radioiododestannylation of tin precursor 17 using (NaI)-I-123 and 0.3% peracetic acid in 84% radiochemical yield in 20 min.