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

用~(18)O(P，n)和~(18)F反应合成了一个简单的钛靶盒。用6-8%浓缩的(^8OJH_2O)样品作为靶材。~(18)F的活度为10~(-12)mCI，是在束流为15~(-12)A的情况下，等待2小时使~(13)N产生衰变而获得的。离子色谱分析表明，载体氟的存在水平为0.1-0.2ppm。AQ的转换。(18F；F)进入反应性亲核试剂，随后的反应在同一血管中进行。在聚甲基戊烯(TPX)容器中的增溶作用导致了与吡喃容器相比，^&lt；18；F的拆分产率更高。我们发现被吸电子取代基活化的苯基二甲基硫甲磺酸盐与(Bu)_4N+~+18&gt；F~-发生亲核取代反应，得到~&lt；~(18&gt；F)~-标记的芳基氟化物。只有在非常活泼的…中，二甲基硫基才能得到合理的产率使用TPC容器的更多d化合物。我们还成功地使用了从这个水目标到脂肪族亲核取代反应的^&lt；18&gt；F-氟化剂。合成NCa2-脱氧-2(2-氟代葡萄糖(2-lt；18；gt；FDG)的合成路线涉及(18；18；gt；在TPX容器中的甲基3-0-benzyl-4，6-3-benzylidene-2-3-trifluoromethanusulfonyl&lt；beta&gt；-D-mannopyranoside上的氟代离子置换，然后用6N HCl水解，产生34-43%的总放射性化学产率，而不防止衰变。这种方法构成了使用氟离子的NCA2-^；18；FDG的替代路线。甲基3，4-0isopropylidene-2-3-trifluoromethanesulfonyl-6-3-teiryl-&lt；beta&gt；-D-talopyranoside与(k/2.2.2.)^&lt；+18&gt；F^-发生亲核氟化反应，再经6N-HCl水解制得2-脱氧-2-(^&lt；18&gt；Fjflo-D-半乳糖)(2-^&lt；18&gt；FDGal)，总放化产率为36-39*，未对衰变进行校正，首次成功合成了使用(^&lt；18&gt；氟离子。较少

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