无载体^131I-MIBG锡试剂前体的合成

Synthesis of a Tin Precursor of Carrier-free ^(131)I-MIBG

目的:探讨合成制备一种无载体^(131)I-MIBG的前体化合物。方法:从简单原料间碘苄胺开始,通过3步反应合成无载体^(131)I-MIBG的锡试剂前体N,N'-二(叔丁氧羰基)-3-(三丁基锡基)-苄胍,用同位素^(131)I标记制备无载体^(131)I-MIBG,测定其标记率。结果:总收率41.5%,经红外光谱、核磁共振谱、质谱进行结构确证,制备的无载体^(131)I-MIBG标记率大于80%。结论:合成了一种合适的锡试剂前体,可以用于制备无载体^(131)I-MIBG。该合成路线收率高,原料易得,反应条件温和,操作简单,适合实验室条件下制备。

Objective： The precursor for the preparation of carrier-free ^131I-MIBG was to be synthesized.Methods： Starting with the easily accessible material metaiodobenzylamine, the precursor N,N＇-bis（tert-butyloxycarbonyl）-3-（tributylstannyl）-benzylguanidine for the preparation of carrier-free ^131I-MIBG was synthesized through three steps of reaction. The radiochemical yield was determined by labelling with isotope^131 I. Results： The total chemical yield was 41.5%. The structure was verified by IR,^1HNMR and MS. The labeling yield was determined to be more than 80%. Conclusions： An ideal tin precursor for the preparation of carrier-free^131I-MIBG has been synthesized. The synthetic route shows high yield and raw material is easy to obtain, the reaction condition is mild and easy in operation. It is suitable for production under laboratory conditions.