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 reactio...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.展开更多
基金the National Natural Science Foundation (39770230) Natural Science Foundation ofJiangsu Province (BK99163) and Department of
文摘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.
