Fully automated synthesis of PET TSPO radioligands [¹¹C]DAA1106 and [¹⁸F]FEDAA1106

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• 作者：Min Wang ; Mingzhang Gao ; Qi-Huang Zheng ; ^{qzheng@iupui.edu}
• 关键词：Translocator protein 18  ; kDa (TSPO) ; [11C]DAA1106 ; [18F]FEDAA1106 ; Positron emission tomography (PET) ; Radiosynthesis ; Automation
• 刊名：Applied Radiation and Isotopes
• 出版年：2012
• 出版时间：June, 2012
• 年：2012
• 卷：70
• 期：6
• 页码：965-973
• 全文大小：591 K

文摘

[¹¹C]DAA1106 was prepared by O-[¹¹C]methylation of DAA1123 with [¹¹C]CH₃OTf and NaH in CH₃CN at 80 ¡ãC and isolated by HPLC combined with SPE purification in 60-70 % decay corrected radiochemical yield. [¹⁸F]FEDAA1106 was synthesized by the nucleophilic substitution of tosyloxy-FEDAA1106 in DMSO with K[¹⁸F]F/Kryptofix 2.2.2 at 140 ¡ãC and isolated by HPLC combined with SPE purification in 30-60 % decay corrected radiochemical yield. The specific activity for [¹¹C]DAA1106 and [¹⁸F]FEDAA1106 was 370-740 GBq/¦Ìmol and 37-222 GBq/¦Ìmol at EOB, respectively.