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Composition enriched in single isomer of NUC-1031 and preparation method and use thereof
Composition enriched in single isomer of NUC-1031 and preparation method and use thereof
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机译:富含nuc-1031单一异构体的组合物及其制备方法和用途
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摘要
Provided is a preparation method of a composition enriched in compound Sp-1. The method performs isomer separation on a reaction product from the first step, and then performs a two-step chemical synthesis, so as to prepare a composition comprising high-purity compound Sp-1, wherein the HPLC purity of the single isomer Sp-1 is 90% or more. Provided is a composition enriched in compound Sp-1. The composition has an inhibitory effect on tumor cell proliferation in vitro significantly higher than that of NUC-1031 and compound Rp-1. Also provided are the use of the composition, and a pharmaceutical composition comprising the composition and at least one pharmaceutically acceptable excipient.
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机译:提供了一种富含化合物S p Sub> -1的组合物的制备方法。该方法从第一步开始对反应产物进行异构体分离,然后进行两步化学合成,以制备包含高纯度化合物S p Sub> -1的组合物,其中HPLC单一异构体S p Sub> -1的纯度为90%以上。提供了富含化合物S p Sub> -1的组合物。该组合物对体外肿瘤细胞的抑制作用明显高于NUC-1031和化合物R p Sub> -1。还提供了该组合物的用途,以及包含该组合物和至少一种药学上可接受的赋形剂的药物组合物。
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