Wang, MinGao, MingzhangXu, ZhidongZheng, Qi-Huang2016-04-222016-04-222015-10Wang, M., Gao, M., Xu, Z., & Zheng, Q.-H. (2015). Synthesis of a PET tau tracer [11C]PBB3 for imaging of Alzheimer’s disease. Bioorganic & Medicinal Chemistry Letters, 25(20), 4587–4592. http://doi.org/10.1016/j.bmcl.2015.08.053https://hdl.handle.net/1805/9391The authentic standard PBB3 and its precursor N-desmethyl-PBB3 as well as TBS-protected N-desmethyl-PBB3 precursor for radiolabeling were synthesized from 5-bromo-2-nitropyridine, acrolein diethyl acetal, 6-methoxy-2-methylbenzothiazole, and diethylchlorophosphate with overall chemical yield 1% in six steps, 2% in five steps, and 1% in six steps, respectively. [11C]PBB3 was prepared from either desmethyl-PBB3 or TBS-protected desmethyl-PBB3 with [11C]CH3OTf through N-[11C]methylation and isolated by HPLC combined with SPE in 20–25% and 15–20% 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.enPublisher Policy[11C]PBB3Tau tracerradiosynthesisArticle