Gao, MingzhangWang, MinGreen, Mark A.Hutchins, Gary D.Zheng, Qi-Huang2015-11-202015-11-202015-05Gao, M., Wang, M., Green, M. A., Hutchins, G. D., & Zheng, Q. H. (2015). Synthesis of [11 C] GSK1482160 as a new PET agent for targeting P2X 7 receptor. Bioorganic & medicinal chemistry letters, 25(9), 1965-1970. http://dx.doi.org/10.1016/j.bmcl.2015.03.021https://hdl.handle.net/1805/7522The authentic standards GSK1482160 and its isomer, as well as the radiolabeling precursors desmethyl-GSK1482160 and Boc-protected desmethyl-GSK1482160 were synthesized from l-pyroglutamic acid, methyl l-pyroglutamate and 2-chloro-3-(trifluoromethyl)benzylamine with overall chemical yield 27–28% in 3 steps, 58% in 4 steps, 76% in 1 step and 33% in 2 steps, respectively. [11C]GSK1482160 was prepared from either desmethyl-GSK1482160 or Boc-protected desmethyl-GSK1482160 with [11C]CH3OTf through N-[11C]methylation and isolated by HPLC combined with SPE in 40–50% and 30–40% radiochemical yield, respectively, based on [11C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the specific activity at EOB was 370–1110 GBq/μmol with a total synthesis time of ∼40-min from EOB.en-USPublisher Policy[11C]GSK1482160radiosynthesispositron emission tomographyArticle