3-[4-(4-[^(18)F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶的放射化学合成  

Radiosyntheses of 3-{[4-(4-[^(18)F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine

作　　者：田海滨[1] 尹端沚[1] 张岚[1] 张春富[1] 李俊玲[1] 周伟[1] 汪勇先[1] 

机构地区：[1]中国科学院上海原子核研究所,上海201800

出　　处：《核技术》2003年第8期628-632,共5页Nuclear Techniques

基　　金：中国科学院创新工程重大项目(KJCXI-SW-08)资助

摘　　要：L-750,667是具有高亲和性(Ki= 0.51 nmol/L)的D4受体选择性配体,采用一锅法用氟[18F]化物放射化学合成了L-750,667的类似物:3-[4-(4-[18F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶。4-氟[18F]苯甲醛是由无载体的 [18F]F-与标记前体4-三甲基铵苯甲醛-三氟甲基磺酸盐在DMSO中反应获得。在同一容器中,4-氟[18F]苯甲醛和3-(哌嗪-1-基)甲基-1H-吡咯并[2,3-b]吡啶完成胺烷基化反应得到产物。产物的纯化使用HPLC,产物保留时间tR=9.4min。在同一条件下,确定产物的放化纯度。放化产率为12.0%,放化纯度>98%,比活度高于37GBq/μmol,全部合成时间(包括高效液相分离)为73min。制备的产物可作为潜在的多巴胺D4受体正电子发射断层(PET)显像剂。L-750,667 is a novel, high-affinity (Ki = 0.51 nmol/L) and selective D4 receptor ligand. A L-750,667 analogue, 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl}methyl-1H-pyrrolo[2,3-b]pyridine, was prepared by reacting 3- (piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine with 4-[18F]fluorobenzaldehyde. The 4-[18F] fluorobenzaldehyde was prepared by nucleophilic substitution using no carrier added [18F]fluoride from trimethylammonium- benzaldehyde triflate in DMSO. The radiochemical yield of 3-{[4-(4-[18F]fluorobenzyl)] piperazin-1-yl}methyl-1H- pyrrolo[2,3-b]pyridine was 12.0% (decay –corrected) with a radiochemical purity better than 98% and a specific activity greater than 37GBq/mmol, and the synthesis time including HPLC purification was 73 min. This labeled compound may be a useful PET tracer for dopamine D4 receptors.

关 键 词：^18F 7-氮杂吲哚类似物 多巴胺D4受体 PET 放化合成 

分 类 号：O615.42[理学—无机化学]