| 袁昊林,吴玉保,杨阳,贺万丽,赵佩佩,汪颖,蔡岩.化学通报,2019,82(11):1013-1018. |
| 甘露糖苷酶抑制剂Kifunensine的改进合成方法研究 |
| An Improved Synthetic Approach to Mannosidase Inhibitor— Kifunensine |
| 投稿时间：2019-06-05 修订日期：2019-08-26 |
| DOI： |
| 中文关键词: Kifunensine 甘露糖苷酶抑制剂 合成改进 |
| 英文关键词:Kifunensine, Mannosidase inhibitor, Improved synthetic method. |
| 基金项目:天津市滨海新区科技计划项目（2014） |
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| 中文摘要: |
| Kifunensine是一种从名为Kitasatosporia kifunense的放线菌中分离出来的生物碱，它是一种中性，稳定的化合物，同时也是甘露糖苷酶I的有效抑制剂，目前被广泛地用于药物研发领域，具有非常高的商业价值，但是它的合成制备非常困难，存在收率低、合成成本高等问题。本文对其合成方法进行了研究，以廉价易得的L-古洛糖酸-γ-内酯为原料，经过一系列转化得到Kifunensine，该操作中多个步骤可以用一锅法投料，操作简便，总产率为4.8%，该方法为该化合物的大规模制备提供了新的思路。 |
| 英文摘要: |
| Kifunensine is a kind of alkaloid which is isolated from Kitasatosporia kifunense. Kifunensine is a neutral and stable compound, it is also the effective inhibitor of mannosidase I. Kifunensine is widely used in the field of pharmaceutical research and development at present, it owns extremely high commercial value. However, the synthesis of Kifunensine meets lots of difficult, the synthetic yield is low and the cost is high. In this article, we reported an improved synthetic method of Kifunensine, this novel method initiated with commercial available L-gulonic acid-γ-lactone, one-pot synthesis protocol has been applied in some of the synthetic steps, the operation is easy to be handle and the total yield can be reached to 4.8%. This novel method provides a probability to the large scale synthesis of Kifunensine. |
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