NCA [F-18] LABELING OF ALIPHATIC-COMPOUNDS IN HIGH YIELDS VIA AMINOPOLYETHER - SUPPORTED NUCLEOPHILIC-SUBSTITUTION
NCA [F-18] LABELING OF ALIPHATIC-COMPOUNDS IN HIGH YIELDS VIA AMINOPOLYETHER - SUPPORTED NUCLEOPHILIC-SUBSTITUTION
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DOI：
10.1002/jlcr.2580230503
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发表时间：
1986-05-01
影响因子：
1.8
通讯作者：
HOLM, U
中科院分区：
文献类型：
--
作者：
BLOCK, D;KLATTE, B;HOLM, U
n.c.a.的亲核引入。- [18 F]-氟化物转化为烷烃和羧酸使用阴离子活化的大环聚醚进行了研究。在双环氨基聚醚APE 2.2.2存在下进行的反应在温和条件下产生了高的放射化学产率（40-65%）。对于成功的18 F标记来说，合适的阳离子/聚醚对很重要，它会在偶极非质子溶剂中产生非溶剂化的[18 F]-氟化物，并确保高离子浓度，从而增强反应性。研究了底物浓度、APE浓度、阳离子、阴离子和水对反应的影响，并对反应条件进行了优化。
The nucleophilic introduction of n.c.a. - [18F]-fluoride into alkanes and carboxylic acids using anion activation by macrocyclic polyethers was investigated. The reactions carried out in the presence of the bicyclic aminopolyether APE 2.2.2 gave rise to high radiochemical yields (40-65%) under mild conditions. Important for the successful 18F-labeling is a suitable cation/polyether couple, which leads to an unsolvated [18F]-fluoride in a dipolar aprotic solvent and ensures a high ion concentration, thus enhancing the reactivity. Reaction parameters, such as concentration of substrate and APE, the influence of cation, anion and water were studied and optimized.