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    • 4. 发明授权
    • Method of preparing rhenium complex using borohydride exchange resin
    • 使用硼氢化物交换树脂制备铼配合物的方法
    • US06888019B1
    • 2005-05-03
    • US10838805
    • 2004-05-04
    • Sang Hyun ParkKyung Bae ParkSun Ju Choi
    • Sang Hyun ParkKyung Bae ParkSun Ju Choi
    • C07F13/00A61K51/00
    • C07F13/005A61K51/0478
    • Disclosed is a method of preparing a rhenium complex by use of a borohydride exchange resin, including dissolving perrhenic acid in a solution containing ethylenediamine tetraacetate, mannitol and stannous chloride to obtain a perrhenic acid solution (step 1), which is then mixed with disulfide in the presence of a borohydride exchange resin and reacts at room temperature, to obtain a rhenium complex (step 2). The preparation method of the current invention is characterized in that rhenium is reduced to have a desired oxidation number through the dissolving of the step 1, whereby the reaction of the step 2 can occur at room temperature. In addition, use of the borohydride exchange resin as a reducing agent results in direct formation of the rhenium complex of sulfide from disulfide, without the need of synthesis of thiol-protected S-precursor. Therefore, radioactive pharmaceuticals having high values can be economically and efficiently produced.
    • 公开了使用硼氢化物交换树脂制备铼络合物的方法,包括将高铼酸溶解在含有乙二胺四乙酸酯,甘露糖醇和氯化亚锡的溶液中以获得高铼酸溶液(步骤1),然后将其与二硫化物混合 硼氢化物交换树脂的存在并在室温下反应,得到铼络合物(步骤2)。 本发明的制备方法的特征在于,通过步骤1的溶解将铼还原成具有所需的氧化数,由此步骤2的反应可以在室温下进行。 此外,使用硼氢化物交换树脂作为还原剂导致硫化物从二硫化物直接形成铼络合物,而不需要合成硫醇保护的S-前体。 因此,具有高价值的放射性药物可以经济有效地产生。