Fully automated synthesis of [18F]T807, a PET tau tracer for Alzheimer's disease

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:25

Article

Gao, Mingzhang¹  Wang, Min¹  Zheng, Qi-Huang¹ 

[1] Indiana Univ Sch Med, Dept Radiol & Imaging Sci, Indianapolis, IN 46202 USA

关键词: [F-18]T807;    Tau tracer;    Automation;    Positron emission tomography (PET);    Alzheimer's disease (AD);   

DOI  :  10.1016/j.bmcl.2015.05.035

来源: Elsevier

【 摘 要 】

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. [F-18]T807 was synthesized from T807P by the nucleophilic [F-18]fluorination with K[F-18]F/Kryptofix 2.2.2 in DMSO at 140 degrees C followed by reduction with Fe powder/HCOOH through manual synthesis with 5-10% decay corrected radiochemical yield in two steps. [F-18]T807 was also synthesized from t-Boc-protected T807P by a concurrent [F-18]fluorination and deprotection with K[F-18]F/Kryptofix 2.2.2 in DMSO at 140 degrees C and purified by HPLC-SPE method in a home-built automated [F-18]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/mu mol. (C) 2015 Elsevier Ltd. All rights reserved.

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