Radiosynthesis of 1-[F]fluoroethyl-L-tryptophan as a novel potential amino acid PET tracer |
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Authors: | Ting Sun Ganghua TangXiaoyan Wang Xianghua ChenZhifeng Chen ShihChen Wang |
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Affiliation: | a Department of Cardiac Function, Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200011, PR China b Department of Nuclear Medicine, the first affiliated hospital, SunYat-Sen University, Guangzhou 510080, PR China c State Key Laboratory of Oncogenes and Related Genes, Shanghai Cancer Institute, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200032, PR China d Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital, 1 Shuaifuyuan Wangfujing Beijing 100730, PR China |
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Abstract: | 18F labeled natural amino acids have been introduced as promising tumor imaging agents. A novel [18F]fluoro amino acid analog 1-[18F]fluoroethyl-L-tryptophan (1-[18F]FETrp) was designed and synthesized by a two-pot three-step procedure, including the synthesis of 1-[18F]fluoro-2- (tosyloxy)ethane, the [18F]fluoroethylation of the precursor N-Boc-L-tryptophan ethyl ester and following the deprotection of the tert-butoxycarbonyl and ethyl ester protecting groups. 1-[18F]FETrp was resulted in 0.9±0.2% (n=5) radiochemical yields (no decay corrected) by HPLC purification, within a total synthesis time of 65 min. The radiochemical purity of 1-[18F]FETrp was 95-97%. The radiosynthetic method needs to be further optimized to get a satisfying radiochemical yield. |
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Keywords: | 1-[18F]FETrp Radiosynthesis Automated PET tracers |
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