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优良的Aβ显像剂必须对Aβ斑块有较高的亲和性,而体外竞争结合实验是筛选Aβ斑块显像剂的有效方法,实验中需要使用放射性配基[125I]TZDM。以对溴苯胺为起始原料,经过四步反应合成了[125I]TZDM的前体化合物Bu3Sn-TZDM,并通过125I进行标记制备了[125I]TZDM,标记率为62.5%。粗产物通过HPLC分离后,获得放射化学纯度大于97%的[125I]TZDM,实际产率为25%。
Excellent A [beta] imaging agents must have a high affinity for A [beta] plaques, whereas in vitro competitive binding assays are an effective method for screening for A [beta] plaque imaging agents that require the use of radioligand [125I] TZDM. The precursor compound Bu3Sn-TZDM of [125I] TZDM was synthesized by 4-step reaction using p-bromoaniline as a starting material. [125I] TZDM was labeled with 125I and the labeling rate was 62.5%. After isolation of the crude product by HPLC, [125I] TZDM with radiochemical purity greater than 97% was obtained with an actual yield of 25%.