Browsing by Subject "Tau tracer"

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    Fully automated synthesis of [18F]T807, a PET tau tracer for Alzheimer’s disease
    (Elsevier, 2015-08) Gao, Mingzhang; Wang, Min; Zheng, Qi-Huang; Department of Radiology and Imaging Sciences, School of Medicine
    The authentic standard T807 and its nitro-precursor T807P as well as t-Boc-protected T807P precursor for radiolabeling were synthesized from (4-bromophenyl)boronic acid, 3-bromo-4-nitropyridine and 3-bromo-6-nitropyridine with overall chemical yield 27% in three steps, 4–7% in three to five steps, and 3–8% in four to five steps, respectively. [18F]T807 was synthesized from T807P by the nucleophilic [18F]fluorination with K[18F]F/Kryptofix 2.2.2 in DMSO at 140 °C followed by reduction with Fe powder/HCOOH through manual synthesis with 5–10% decay corrected radiochemical yield in two steps. [18F]T807 was also synthesized from t-Boc-protected T807P by a concurrent [18F]fluorination and deprotection with K[18F]F/Kryptofix 2.2.2 in DMSO at 140 °C and purified by HPLC-SPE method in a home-built automated [18F]radiosynthesis module with 20–30% decay corrected radiochemical yield in one step. The specific activity of [18F]T807 at end of bombardment (EOB) was 37–370 GBq/μmol.
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    Synthesis of a PET tau tracer [11C]PBB3 for imaging of Alzheimer’s disease
    (Elsevier, 2015-10) Wang, Min; Gao, Mingzhang; Xu, Zhidong; Zheng, Qi-Huang; Department of Radiology and Imaging, IU School of Medicine
    The 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.