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Fully automated synthesis of PET TSPO radioligands [11C]DAA1106 and [18F]FEDAA1106
Authors:Wang Min  Gao Mingzhang  Zheng Qi-Huang
Affiliation:Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202-2111, USA.
Abstract:[(11)C]DAA1106 was prepared by O-[(11)C]methylation of DAA1123 with [(11)C]CH(3)OTf and NaH in CH(3)CN at 80°C and isolated by HPLC combined with SPE purification in 60-70% decay corrected radiochemical yield. [(18)F]FEDAA1106 was synthesized by the nucleophilic substitution of tosyloxy-FEDAA1106 in DMSO with K[(18)F]F/Kryptofix 2.2.2 at 140°C and isolated by HPLC combined with SPE purification in 30-60% decay corrected radiochemical yield. The specific activity for [(11)C]DAA1106 and [(18)F]FEDAA1106 was 370-740GBq/μmol and 37-222GBq/μmol at EOB, respectively.
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