Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [18F]-T808, a PET tau tracer for Alzheimer's disease

被引：23

作者：

Gao, Mingzhang ^{[1
]}

Wang, Min ^{[1
]}

Zheng, Qi-Huang ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 01期

关键词：

F-18]-T808; Tau tracer; Automation; Positron emission tomography (PET); Alzheimer's disease (AD); RADIOPHARMACEUTICALS; OPTIMIZATION; PATHOLOGY; AGENTS;

D O I：

10.1016/j.bmcl.2013.11.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The authentic standard T808 and its corresponding mesylate precursor T808P were synthesized in six steps using ethyl vinyl ether and trichlorocetyl chloride as starting materials. The overall chemical yields of T808 and T808P were 35% and 52%, respectively. [F-18]-T808 was synthesized from T808P by the nucleophilic substitution with K[F-18]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 35-45% radiochemical yield with 37-370 GBq/mu mol specific activity at end of bombardment (EOB). (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：254 / 257

页数：4

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