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Development of a Target Box for the production of 18F and its Conversion into reactive reaguents for Clinical Use

开发用于生产 18F 的靶盒并将其转化为临床使用的反应试剂

基本信息

批准号：
60870037
负责人：
KOJIMA Masaharu
金额：
$ 5.76万
依托单位：
Kyushu Nuversity
依托单位国家：
日本
项目类别：
Grant-in-Aid for Developmental Scientific Research
财政年份：
1985
资助国家：
日本
起止时间：
1985 至 1987
项目状态：
已结题

项目摘要

A simple titanuim target box has been constucted for the profuction of^<18>F via^<18>O(P,n)^<18>F reaction. A 6-8% enriched sample of (^8OJH_2O was used as target meterial. The^<18>F activety of 10-12 mci was obtained by a 20 min irradation with a beam current of 15 <micru>A after waiting 2 hr to alloe^<13>N produced concomitantly ot decay. Ion chromatographic analsys showed that carrier fluoride is present at the level of 0.1-0.2 ppm. The conversion of the aq. (^<18>Flfuoride into reactive nucleophilic reagents and the subsequent reaction was pwrformed in the same vassel. Resolubilization in a Polymewthlpentene(TPX) vessel resulted in a higher resolubilization yield for the^<18>F when compared to a pyrex vessel. We have found that phenyldimathylsulfonium methylsulfactes activeted by electron-withdrawing substituents undergo nuclecophilic substitutuon with (Bu)_4N+^<+18>F^- to give^<18>F-labeled aryl fluorides. This dimethylsulfonium group allows reasonable yeilds only in very activate … More d compounds using a TPC vessel. We have also been successful in the use of^<18>F-fluorinating agents from this water target to aliphatic nucleophilic substitution reactions. A syntrhetic route to NCA 2-deoxy-2(^<18>Fjfluoro-glucose (2-^<18>FDG) involving (^<18>Flfuoride ion displacement on methyl 3-0-benzyl-4,6-3-benzylidene-2-3-trifluoromethanusulfonyl<beta>-D-mannopyranoside in a TPX vessel followed by hydrolysis with 6N HCl produces a 34-43% overall rediochemaicl yiels without corretion for decay. This methodology constitutes an alternative route to NCA 2-^<18>FDG using (^<18>Flfluoride ion. A nucleophilic rafiofulorination of methyl 3,4-0isopropylidene-2-3-trifluoromethanesulfonyl-6-3-teiryl-<beta>-D-talopyranoside with (k/2.2.2.)^<+18> F^- followed by hydrolysis with 6N HCl afforded 2-deoxy-2-(^<18>Fjfluoro-D-galactose (2-^<18>FDGal) in 36-39* overall radiochemical yield without correction fot decay, proveding the first successful synyhesis of NCA 2-^<18>FDGal using (^<18>Fjfluoride ion. Less

本文报道了一个简单的钛靶盒，用于<18>由^<18>O（P，n）^<18>F反应制备^ F。以富集6-8%的（^8O_2H_2O）样品为靶物质。用<18>15 A的束流照射20分钟<micru>，等待2小时以消除<13>伴随衰变产生的^-N，得到10-12毫居里的^-F活度。离子色谱分析表明，载体氟含量为0.1- 0.2ppm。水的转化。（2）<18>氟化物转化为反应性亲核试剂，随后的反应在同一容器中进行。与派热克斯玻璃容器相比，在聚甲基戊烯（TPX）容器中的再溶解导致13 F的更高的再溶解产率<18>。我们发现，在吸电子取代基的作用下，苯基二甲基锍甲基磺酸盐与（Bu）_4N+^<+18>F^-发生亲核取代反应，生成了^<18>F-标记的芳基氟化物。这种二甲基锍基团仅在非常活跃的情况下才允许合理的产率 ...更多信息 d化合物使用TPC容器。我们还成功地将13 <18>F-氟化剂从该水靶向脂肪族亲核取代反应中使用。NCA 2-脱氧-2-<18>氟-葡萄糖（2-β <18>FDG）的合成路线包括<18>在TPX容器中在甲基3-O-苄基-4，6 -3-亚苄基-2 -3-三氟甲磺酰基<beta>-D-吡喃甘露糖苷上的（2-β）氟离子置换，然后用6 N HCl水解，产生34-43%的总放射化学产率，而没有衰变的校正。该方法构成了使用（3F）氟化物离子的NCA 2- 13 FDG的替代途径<18><18>。3，4 - 0-异亚丙基-2-（3-三氟甲磺酰基）-6-（3-硬脂酰基）-<beta>β-D-Talopyranoside与（k/2.2.2.）在不校正衰变的情况下，以36-39* 的总放射化学产率得到2-脱氧-2-（3F）-<18>氟-D-半乳糖（2-β <18>FDGal），证明了使用（3F）氟化物离子首次成功合成NCA 2-β <18>FDGal<18>。少