3-(4-[^(18)F]氟苄基)-8-羟基-1,2,3,4-四氢苯并吡喃[3,4-c]吡啶-5-酮的放射化学合成  

Synthesis of 3-(4-[^(18)F] fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one

作　　者：李谷才[1] 尹端沚[1] 程登峰[1] 王明伟[1] 郑明强[1] 汪勇先[1] 

机构地区：[1]中国科学院上海应用物理研究所放射性药物研究中心,上海201800

出　　处：《核技术》2006年第5期368-371,共4页Nuclear Techniques

基　　金：国家自然科学基金资助项目(30371634);中国科学院创新工程重大资助项目(KJCXI-SW-08)

摘　　要：多巴胺D4受体是一种G蛋白偶联受体,在精神分裂症病因发展中起着重要作用。通过核医学显像仪器,利用PET显像剂可以确定受体在活体内的分布、含量变化等。本文用三氟甲基磺酸-4-三甲基铵苯甲醛作标记前体,采用“一锅法”制备了一种潜在的多巴胺D4受体PET显像剂3-(4-[18F]氟苄基)-8-羟基-1,2,3,4-四氢苯并吡喃[3,4-c]吡啶-5-酮(18F-FHTP)。其总的合成时间为105min,放射化学产率为19.7%,比活度大于120GBq/μmol。Dopamine D4 receptor is a G-protein coupled receptor and it is hypothesized to relate with the pathophysiology and pharmacotherapy of schizophrenia while its level in brain regions is much lower. With the help of nuclear medicine imaging technology and suitable imaging agents, the receptors＇ distribution and the level variation can be determined in living bodies. In this article we describe the synthesis of a putative dopamine D4 receptor radioli- gand, 3-（4-[^18F]fluorobenzyl）-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c] pyridin-5-one （ISF-FHTP） from 4-trimethylammoniumbenzaldehyde triflate through a two-steps one-pot procedure with a total radiochemical yield of 19.7% （decay-correctgd）. The radiochemical synthesis of ^18F-FHTP took about 105 min and its specific activity was greater than 120GBq/μmol.

关 键 词：苯并吡喃[3 4-c]吡啶-5-酮 氟-18 放射化学合成 多巴胺D4受体 

分 类 号：O621.3[理学—有机化学]