摘要
The ligand of N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4’-iodophenyl) nortropane (FP-β-CIT) and mesylate precursor were synthesized by hydrolysis of cocaine, followed by dehydration, esterification, Grignard reaction, N-demethylation, iodination, N-alkylation with 3-bromopropanol and methylsulfonylation. Finally, 18F-FP-β-CIT was prepared by nucleophilic fluorination of the mesylate with K18F/K2.2.2 (Kryptofix). The labeling yield of 18F-FP-β-CIT is 25%~30%. The total radiochemical yield of this compound, calculated from the end of bombardment (EOB) with decay correction, is 10%~12% with a synthesis time of 100~110.min. The radiochemical purity of 18F-FP-β-CIT is greater than 90%, and this compound in aqueous solution is also stable for more than 4 hours at room temperature. It is stable enough for clinical study.
The ligand of N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4'-iodophenyl) nortropane (FP-β-CIT) and mesylate precursor were synthesized by hydrolysis of cocaine, followed by dehydration, esterification, Grignard reaction, N-demethylation, iodination, N-alkylation with 3-bromopropanol and methylsulfonylation. Finally, 18F-FP-β-CIT was prepared by nucleophilic fluorination of the mesylate with K18F/K2.2.2 (Kryptofix). The labeling yield of 18F-FP-β-CIT is 25%~30%. The total radiochemical yield of this compound, calculated from the end of bombardment (EOB) with decay correction, is 10%~12% with a synthesis time of 100~110.min. The radiochemical purity of 18F-FP-β-CIT is greater than 90%, and this compound in aqueous solution is also stable for more than 4 hours at room temperature. It is stable enough for clinical study.
基金
the National Natural Science Foundation (39770230)
Natural Science Foundation ofJiangsu Province (BK99163) and Department of
关键词
大脑分子
柯卡因衍生物
托烷衍生物
成象剂
Cocaine derivatives, Tropane derivatives, Dopamine Transporter, FP-β- CIT, Imaging agent
