Miao, CaihongDong, FuguiJia, LimengLi, WeiWang, MinZheng, Qi-HuangXu, Zhidong2019-04-042019-04-042019-05Miao, C., Dong, F., Jia, L., Li, W., Wang, M., Zheng, Q.-H., & Xu, Z. (2019). Radiosynthesis of a carbon-11-labeled AMPAR allosteric modulator as a new PET radioligand candidate for imaging of Alzheimer’s disease. Bioorganic & Medicinal Chemistry Letters, 29 (10), 1177-1181. https://doi.org/10.1016/j.bmcl.2019.03.027https://hdl.handle.net/1805/18777To develop PET tracers for imaging of Alzheimer’s disease, a new carbon-11-labeled AMPAR allosteric modulator 4-cyclopropyl-7-(3-[11C]methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide ([11C]8) has been synthesized. The reference standard 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide (8) and its corresponding desmethylated precursor 4-cyclopropyl-7-(3-hydroxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide (9) were synthesized from 4-methoxyabiline and chlorosulfonyl isocyanate in eight and nine steps with 3% and 1% overall chemical yield, respectively. The target tracer [11C]8 was prepared from the precursor 9 with [11C]CH3OTf through O-[11C]methylation and isolated by HPLC combined with SPE in 10–15% radiochemical yield, based on [11C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the molar activity (AM) at EOB was 370–740 GBq/μmol with a total synthesis time of 35–40-minutes from EOB.enPublisher Policyα-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptorcarbon-11-labeled AMPAR allosteric modulatorradiosynthesisArticle