Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor
Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor
复制标题
DOI：
10.1039/b407938h
复制
发表时间：
2004-01-01
期刊：
影响因子：
6.1
通讯作者：
Pike, VW
中科院分区：
文献类型：
--
作者：
Lu, SY;Watts, P;Pike, VW
在流体动力驱动的微反应器中，成功地用两种短寿命正电子发射体（碳 11 或氟 18）之一标记了羧酸酯。室温下得到非放射性甲酯4a；其产量随着底物浓度的升高和输注速度的降低而增加。 1 (10 mM) 与 2b 在输注速率为 10 μL min(-1) 时反应得到放射性甲酯 4b，衰减校正放射化学产率 (RCY) 为 56%，当输注速率降低至 1 μL min(-1) 时，RCY 增加至 88%。从1和3a合成非放射性氟乙酯5a需要在加热块上将微反应器加热到80℃（14-17％RCY），而从1和3b得到相应的放射性5b，在10％RCY中。放射性“外周”苯二氮卓受体配体7b是通过酸6与标记剂2b在45％RCY中以10μL min(-1)的输注速率反应获得的。当输注速度减少至1μL·min(-1)时，RCY增加至65%。结果例证了一种生产用于正电子发射断层扫描成像的放射性示踪剂的新方法，该方法具有许多潜在的优点，包括需要少量底物、增强反应、快速反应优化和易于产物纯化。
Carboxylic esters were successfully labeled with one of two short-lived positron-emitters, carbon-11 or fluorine-18, within a hydrodynamically-driven micro-reactor. The non-radioactive methyl ester 4a was obtained at room temperature; its yield increased with higher substrate concentration and with reduced infusion rate. Radioactive methyl ester 4b was obtained from the reaction of 1 (10 mM) with 2b in 56% decay-corrected radiochemical yield (RCY) at an infusion rate of 10 muL min(-1), and when the infusion rate was reduced to 1 muL min(-1), the RCY increased to 88%. The synthesis of the non-radioactive fluoroethyl ester 5a from 1 and 3a required heating of the micro-reactor on a heating block at 80 degreesC (14-17% RCY), whilst the corresponding radioactive 5b from 1 and 3b was obtained in 10% RCY. The radioactive 'peripheral' benzodiazepine receptor ligand 7b was obtained from the reaction of acid 6 with labeling agent 2b in 45% RCY at an infusion rate of 10 muL min(-1). When the infusion rate was reduced to 1 muL min(-1), the RCY increased to 65%. The results exemplify a new methodology for producing radiotracers for imaging with positron emission tomography that has many potential advantages, including a requirement for small quantities of substrates, enhanced reaction, rapid reaction optimisation and easy product purification.