多巴胺转运蛋白显像剂~(18)F-FP-β-CIT的制备

Preparation of ~(18) F-FP-β-CIT as a PET Imaging Agent

摘要: 可卡因经水解、脱水、甲酯化、苯基溴镁格氏反应、脱 N-甲基、碘化、N烷基化、甲磺酰化等反应制备氟标记前体, 用 K2 2 2 催化进行氟标记, 得到 18F- FP- β- CITN- (3-氟丙基 ) - 2 β-甲酯基 - 3β- (4'-碘苯 )去甲基托烷,标记率 2 5%～ 30 %, 放射化学产率 10 %～ 12 %, 合成及纯化时间 10 0～ 110 min,纯化后放化纯度 >95%, 稳定性较好

Abstract: The ligand of N (3 fluoropropyl) 2β carbomethoxy 3β (4' iodophenyl)nortropane (FP β CIT) and mesylate precursor are synthesized by hydrolysis of cocaine, followed by dehydration, esterification, Grignard reaction, N demethylation,iodination,N alkylation with 3 bromopropanol and methylsulfonylation. Finally, 18 F FP β CIT is prepared by nucleophilic fluorination of the mesylate with K 18 F/K 222 (Kryptofix). The labeling yield is 25%～30%, and the total radiochemical yield is 10%～12%. After purifying the radiochemical purity of 18 F FP β CIT is greater than 95%, and stable for more than 4 hours at room temperature. The whole process (including synthesis and analysis) takes only 100~110 minutes.