Synthesis of [18F]-N-3-fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl) nortropane([18F]-FP-β-CIT)

Synthesis of [¹⁸F]-N-3-fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl) nortropane([¹⁸F]-FP-β-CIT)

FANG Ping，

CHEN Zheng-Ping，

LIN Yan-Song，

ZHOU Xian，

DU Yi-Kui，

WANG Shi-Zhen

Nuclear Science and Techniques

Vol.12, No.2

pp.105-110

Published in print 01 May 2001

CLC：O621.3+5, O628.5+1, O629.7, R817.9

21300

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/K_2.2.2 (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 100~110min. 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.

Cocaine derivativesTropane derivativesDopamine TransporterFP-β-CITImaging agent

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