【摘要】 目的合成新的¹¹C 标记小分子苯并呋喃衍生物并研究其生物学性质。方法合成前体5-溴2-（4-胺基苯）苯并呋喃,用改良的¹¹CH₃I 法标记,生成5-溴-2-(4-N-¹¹C-甲胺基苯)-苯并呋喃,以柱色层法测标记率。正常小鼠尾静脉注射5-溴-2-(4-N-¹¹C-甲胺基苯)-苯并呋喃后不同时间处死,测每克组织百分注射剂量率（%ID/g）。结果改良¹¹CH₃I 法标记率为45%,放化纯大于95%。小鼠尾静脉注射药物后,放射性主要分布于肝和肾内,药物能迅速被脑摄取,2 min 达到3.2%ID/g,正常脑对其清除快于对碘的取代物,2与30 min 放射性摄取比值为1.34。结论 ¹¹C 标记小分子溴取代苯并呋喃衍生物,可作为β-淀粉样蛋白（Aβ）显像剂,其生物学性质明显优于碘的取代物。更多还原

【Abstract】 Objective Deposit of β-amyloid protein（Aβ）as senile plaque is one of the patho- physiologic features in Alzheimer’s disease.Several new derivatives of benzofuran were synthesized,¹¹C la- belled,and tested as the potential imaging agents for targeting amyloid deposit.Methods 5-Br-2-（4-amin- ophenyl）benzofuran was synthesized and labelled by an improved method,in which the precursors were mixed with ¹¹CH₃I and dimethyl sulfoxide（DMSO）solution to get 5-Br-2-(4-N-¹¹C-methylaminophenyl) benzofuran.The column method was employed to measure the labelling yields.The biodistribution of the product was studied in 9 normal mice.The characters of the precursor were confirmed by ¹H NMR.Results The labelling yield was 45% with the author’s improved method used in the current study.The radiochemi- cal yield was over 95%.Most of the radioactivity was observed in liver and kidney after intravenous injec- tion.The peak uptake in normal mice brain（3.2 % ID/g）was noted at 2 rain post-injection with a washout faster for 5-Br-substituent than 5-I-substituent.The 2/30 rain ratio of cerebral uptake was 1.34.Conclu- sion The new derivative,¹¹C labelled 5-Br-substituent,showed certain characteristics more favorable than literature reported 5-I-substituent as an Aβ imaging agent.更多还原