取代杯[6]芳烃的制备及在~（18）F-FET制备中的应用

本工作制备了相转移催化剂取代杯[6]芳烃：对磺酸杯[6]芳烃和对叔丁基杯[6]芳烃,并以其为催化剂进行了18F-FET的制备。结果表明,对磺酸杯[6]芳烃作催化剂不仅能够催化FET前体的19F取代反应,而且能够催化FET前体对（对甲苯磺酸酯）乙基苯甲酰（BOC）氨基酸酯的18F标记反应,放化产率为11%。而对叔丁基杯[6]芳烃对催化FET前体的19F取代反应和18F的标记反应均没有催化活性。对磺酸杯[6]芳烃的催化作用可能与它的磺酸基参与络合反应,增大了杯[6]芳烃极性等因素有关。虽然对磺酸杯[6]芳烃催化FET前体的放化产率远低于Kryptofix 2.2.2,但该研究对优化条件找出更好的取...

Full description

Saved in:
Bibliographic Details
Published in同位素 Vol. 24; no. 3; pp. 166 - 171
Main Author 彭程 马云川 陈萧萧 李桂霞 李石磊 张淑婷 贺勇 齐传民
Format Journal Article
LanguageChinese
Published 师范大学化学学院,北京100875 2011
首都医科大学宣武医院PET中心,北京00053%教育部放射性药物化学重点实验室
Subjects
18F
18F-FET
杯芳烃
18F-FET
杯芳烃
18F
Online AccessGet full text
ISSN1000-7512

Cover

More Information
Summary:本工作制备了相转移催化剂取代杯[6]芳烃：对磺酸杯[6]芳烃和对叔丁基杯[6]芳烃,并以其为催化剂进行了18F-FET的制备。结果表明,对磺酸杯[6]芳烃作催化剂不仅能够催化FET前体的19F取代反应,而且能够催化FET前体对（对甲苯磺酸酯）乙基苯甲酰（BOC）氨基酸酯的18F标记反应,放化产率为11%。而对叔丁基杯[6]芳烃对催化FET前体的19F取代反应和18F的标记反应均没有催化活性。对磺酸杯[6]芳烃的催化作用可能与它的磺酸基参与络合反应,增大了杯[6]芳烃极性等因素有关。虽然对磺酸杯[6]芳烃催化FET前体的放化产率远低于Kryptofix 2.2.2,但该研究对优化条件找出更好的取代杯[6]芳烃催化剂具有重要的指导意义。
Bibliography:11-2566/TL
calix[6]arene; 18F; 18F-FET
PENG Cheng,MA Yun-chuan,CHEN Xiao-xiao,LI Gui-xia,LI Shi-lei,ZHANG Shu-ting,HE Yong,QI Chuan-min（1.PET Center,Xuanwu Hospital,Capital Medical University,Beijing 100053,China;2.Key Laboratory of Radiophamaceutical（Beijing Normal University）,College of Chemistry,Beijing Normal University,Beijing 100875,China）
The phase transfer catalyst Substituted Calix[6]arene was preparaed and it was used as catalyst to prepare the tumor diagnostic drug 18F-FET.The results showed that para-sulfonated-calix[6]arene not only catalyzes 19F substitution reaction,but also catalyzes 18F labelling reaction with radiochemical yield of 11%.However,para-tert-butyl-calix[6]arene has no catalytic activity for the 19F substitution reaction nor the 18F labelling reaction of the precursor of FET.The catalyzing of para-sulfonated-calix[6]arene may be related to it＇s sulfonate groups,which participated in the coordination reaction and increased the polarity of calix[6]arene and so on.Although radiochemical
ISSN:1000-7512