Automated Synthesis of 5-HT1A Receptors Antagonists 11C-WAY-100635

A fully automated synthesis of 11C-labeled-N-［2-［4-(2-methoxyphenyl)-1-piperazinyl］ethyl］-N-2-pyridinylcyclohexanecarboxamide maleate (11C-WAY-100635) for imaging 5-HT1A receptors was performed on a module system. 11C-WAY-100635 was obtained based on the methylation reaction of the precursor (O-deme...

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Bibliographic Details
Published inTong wei su Vol. 30; no. 2; pp. 119 - 124
Main Author LI Hui-qiang1,2;ZHEN Zhi-fei1;ZHANG Wei-feng1;LIAO Shu-guang1;LI Hong-li3;XU Jun-ling1,2
Format Journal Article
LanguageChinese
Published Editorial Board of Journal of Isotopes 01.02.2017
Subjects
11c-way-100635 automated synthesis hplc purification
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Summary:A fully automated synthesis of 11C-labeled-N-［2-［4-(2-methoxyphenyl)-1-piperazinyl］ethyl］-N-2-pyridinylcyclohexanecarboxamide maleate (11C-WAY-100635) for imaging 5-HT1A receptors was performed on a module system. 11C-WAY-100635 was obtained based on the methylation reaction of the precursor (O-demethyl)-WAY-100635, purification with HPLC and subsequent removal of organic solvents using a Sep-Pak Plus C18. The results revealed that fully automated synthesis of 11C-WAY-100635 was completed within the total synthesis time of about 40 min. The uncorrected radiochemical yield was between 10% and 20%, and the radiochemical purity was over 97%. After the intravenous injection of 11C-WAY-100635 (about 111 MBq), the uptake in the brain tissues of the white rabbit was significantly higher than the other tissues of head. This method provides simple synthesis of 11C-WAY-100635 with relatively short radiosynthesis time and a high radiochemical yield for clinical need.
ISSN:1000-7512
1000-7512
DOI:10.7538/tws.2016.youxian.036