摘要
8 甲氧基 3 (4 氟苄基) 1,2,3,4 四氢苯并吡喃[3,4 c]吡啶 5 酮(FMTP)作为选择性多巴胺D4受体拮抗剂显示出高的亲和性和选择性(与D4受体的结合常数Ki=4.3nmol/L,与D2受体的结合常数Ki>5800nmol/L)。文章采用三氟甲基磺酸 4 三甲基铵苯甲醛为前体,完成了18F标记的亲核取代反应,用18F标记的中间体同8 甲氧基 1,2,3,4 四氢苯并吡喃[3,4 c]吡啶 5 酮完成胺烷基化反应,得到目标产物8 甲氧基 3 (4 [18F]氟苄基) 1,2,3,4 四氢苯并吡喃[3,4 c]吡啶 5 酮(18F FMTP)。产物的总合成时间(包括高效液相纯化)为110min,放化产率为19.5%,放化纯度大于98%,比活度高于37GBq/μmol。
fluorobenzyl)-8-methoxy-1,2,3,4-tetrahydr ochromeno[3,4- c ]pyridin-5-one(FMTP), a selective D 4 receptor antagonist, exhibits nanomolar affinity and high selectivity. 18 F-FMTP is synthesized in multistep reactions in which fluorine-18 is introduced by nucleophilic halogen displacement on a quaternary ammonium group precursor. The fluorine-18 labeled intermediate is subsequently reductively aminated with 8-methoxy-1,2,3,4-tetrahydrochromeno[3,4- c ]pyridin-5-one to form the final products. The radiosynthesis of 18 F-FMTP needs approximatively 110 min with an overall radiochemical yield of 19.5%(decay-corrected) and with highly effective specific activities(>37 GBq/μmol). 18 F-FMTP may be a useful positron emission tomography (PET) tracer that can be applied to map brain dopamine D 4 receptor.
出处
《核化学与放射化学》
CAS
CSCD
北大核心
2003年第3期151-155,共5页
Journal of Nuclear and Radiochemistry
基金
国家自然科学基金资助项目(10075073)
中国科学院创新工程重大资助项目(KJCXI SW 08)
