中文摘要：

为了找到适合单光子计算机发射断层（SPECT）的脑内β淀粉样蛋白（Aβ）斑块的显像剂，合成了2-（3＇-三正丁基锡-4＇-甲氨基苯基）-6-羟基苯并噻唑，并采用双氧水标记法进行了^131I标记，得到了2-（3’-碘-4＇-甲氨基苯基）-6-羟基苯并噻唑（3＇-^131I-PIB），放化纯大于95％。对文献中原料与条件作了相应的改进，提高了合成的回收率。正常小鼠体内分布实验表明，3＇-^131I-PIB在2min和60min时，小鼠脑摄取分别为（2．45±0．43）％ID／g和（0．19±0．02）％ID／g。说明3＇-^131I-PIB在小鼠脑中初摄取高，清除很快。如果改用合适的核素标记，3＇-I-PIB将是一个有研究前景的Aβ斑块显像剂。

英文摘要：

The synthesis and biodistribution of β-amyloid plaques imaging agent 2-（3＇-iodo-4＇- methylaminophenyl）-6-hydroxy-benzothialzole（3＇-^131I-PIB） were reported. The chemical structure of the labeling precursor 2-（ 3＇-tributylstannyl-4＇-methylaminophenyl ）-6-hydroxybenzothialzole and all its intermediates were verified by ^1H NMR and MS. The radioiodinated compound was prepared using iododestannylation reaction by hydrogen peroxide. Final radiochemical purity is above 95% determined by TLC. The in vivo biodistribution of 3＇-^131I-PIB in normal mice shows excellent brain uptake and washout, indicating this benzothiazole （BTA） derivative has potential for in vivo imaging amyloid deposits.