多巴胺转运蛋白显像剂β-CIT的合成及其碘标记

Synthesis and Iodine Labelling of β-CIT as a Dopamine Transporter Imaging Agent

摘要: 报道了β- CIT(2β-甲酯基 - 3β- (4’-碘苯基 )托烷 )及标记前体 (2β-甲酯基 - 3β- (4’- (三丁基锡 )苯基 )托烷 )的合成路线, 化合物 IR、NMR、MS、元素分析等数据与结构相符, 由标记前体制备 12 5/ 13 1I- β-CIT,标记率和放化纯度均 >90 %。

Abstract: carbomethoxy 3β (4′ iodophenyl)tropane(β CIT) and it's iodine labelling precursor 2β carbomethoxy 3 β(4′ tribuylstannylphenyl)tropane are synthesized, and the chemical structures are confirmed by IR, NMR, MS and elemental analysis. The radiochemical purity of 125 I β CIT and 131 I β CIT are over 90% evaluated by HPLC and TLC.