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    • 5. 发明公开
    • METHOD FOR SOLID-PHASE SYNTHESIS OF DNA-ENCODED CHEMICAL LIBRARY
    • 一种编码DNA的化学文库的固相合成方法
    • EP3284851A1
    • 2018-02-21
    • EP16779596.2
    • 2016-04-13
    • Hitgen Ltd.
    • LI, JinWAN, JinqiaoLIU, GuansaiZHONG, LinaCHEN, YangWANG, ZhiLIU, XinchengMU, YunDOU, Dengfeng
    • C40B40/06C40B20/04C40B70/00C40B50/04C40B50/16
    • C12N15/1068C12P19/34C40B20/04C40B40/06C40B50/04C40B50/16C40B70/00
    • The present invention provides a method of solid-phase synthesis of DNA-encoded compound library. The method includes following steps: a) reacting solid carrier G-1 with linker molecule L-1 to prepare L-G-1; b) reacting DNA with linker molecule L-0 to prepare L-2; c) reacting L-G-1 with L-2 to prepare L-G-2; d) removing protection group of the L-G-2 and obtaining L-G-2-1; e) reacting the L-G-2-1 with synthetic building block and performing DNA encoding; and f) removing the solid carrier and obtaining the DNA-encoded compound library. Compared with the prior art, the present invention can complete post-treatment purification of the reaction only by filtration and irrigation processes for several times. The present invention is simple to operate, can shorten the production cycle of DNA encoded compound library with more than 50%, significantly increases the production efficiency and the unicity as well as the purity of the final products. Besides, the present invention has a high economic value, which is suitable for industrial application.
    • 本发明提供了DNA编码的化合物文库的固相合成方法。 该方法包括以下步骤:a)使固体载体G-1与接头分子L-1反应以制备L-G-1; b)使DNA与接头分子L-0反应以制备L-2; c)使L-G-1与L-2反应以制备L-G-2; d)除去L-G-2的保护基并得到L-G-2-1; e)使L-G-2-1与合成结构单元反应并进行DNA编码; 和f)除去固体载体并获得DNA编码的化合物文库。 与现有技术相比,本发明只需通过过滤和冲洗过程就可以完成反应的后处理纯化数次。 本发明操作简单,可将DNA编码化合物文库的生产周期缩短50%以上,大大提高了生产效率和单一性以及最终产品的纯度。 此外,本发明具有很高的经济价值,适用于工业应用。