同位素
同位素
동위소
ISOTOPES
2001年
1期
6-10
,共5页
方平%陈正平%林岩松%周翔%杜宜奎%王世真
方平%陳正平%林巖鬆%週翔%杜宜奎%王世真
방평%진정평%림암송%주상%두의규%왕세진
多巴胺转运蛋白显像剂%FP-β-CIT%制备
多巴胺轉運蛋白顯像劑%FP-β-CIT%製備
다파알전운단백현상제%FP-β-CIT%제비
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K222催化进行氟标记，得到18F-FP-β-CIT[N-(3-氟丙基)-2β-甲酯基-3β-(4'-碘苯)去甲基托烷]，标记率25%～30%，放射化学产率10%～12%，合成及纯化时间100～110min，纯化后放化纯度>95%，稳定性较好。
可卡因經水解、脫水、甲酯化、苯基溴鎂格氏反應、脫N-甲基、碘化、N烷基化、甲磺酰化等反應製備氟標記前體，用K222催化進行氟標記，得到18F-FP-β-CIT[N-(3-氟丙基)-2β-甲酯基-3β-(4'-碘苯)去甲基託烷]，標記率25%～30%，放射化學產率10%～12%，閤成及純化時間100～110min，純化後放化純度>95%，穩定性較好。
가잡인경수해、탈수、갑지화、분기추미격씨반응、탈N-갑기、전화、N완기화、갑광선화등반응제비불표기전체，용K222최화진행불표기，득도18F-FP-β-CIT[N-(3-불병기)-2β-갑지기-3β-(4'-전분)거갑기탁완]，표기솔25%～30%，방사화학산솔10%～12%，합성급순화시간100～110min，순화후방화순도>95%，은정성교호。
The ligand ofN-(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, 18F-FP-β-CIT is prepared by nucleophilic fluorination of the mesylate with K18F/K222(Kryptofix). The labeling yield is 25%～30%, and the total radiochemical yield is 10%～12%. After purifying the radiochemical purity of 18F-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.
