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Citation: Yuan Haolin, Wu Yubao, Yang Yang, He Wanlin, Zhao Peipei, Wang Ying, Cai Yan. An Improved Synthetic Approach to Mannosidase Inhibitor-Kifunensine[J]. Chemistry, ;2019, 82(11): 1013-1018. shu

An Improved Synthetic Approach to Mannosidase Inhibitor-Kifunensine

Yuan Haolin ² ,
Wu Yubao ² ,
Yang Yang ² ,
He Wanlin ¹ ,
Zhao Peipei ^1,, ,
Wang Ying ^3,, ,
Cai Yan ^1,,

1.
Tianjin International Joint Academy of Biomedicine, Tianjin 300457
2.
College of Pharmacy, Nankai University, Tianjin 300071
3.
Tianjin Crops Research Institute, Tianjin Academy of Agricultural Sciences, Tianjin 300384

Corresponding author: Zhao Peipei, zhaopp_89@163.com Wang Ying, wangying1412@163.com Cai Yan, caiyan_86@163.com
Received Date: 5 June 2019
Accepted Date: 26 August 2019

Figures(2)

Kifunensine is an alkaloid isolated from actinomycetes named Kitasatosporia kifunense. It is a neutral and stable compound, and an effective inhibitor of mannosidase I. Kifunensine is currently widely used in the field of drug discovery and has very high commercial value. However, the synthesis of Kifunensine is difficult, and there are problems such as low yield and high synthesis cost. In this paper, the cheap and easily available L-gulonic acid-γ-lactone was used as a raw material to obtain Kifunensine through a series of reactions. One-pot synthesis protocol has been applied in some of the synthetic steps, which makes the operation simple, and the total yield is 4.8%. This novel method provides a probability to the large scale synthesis of Kifunensine.
- Kifunensine,
- Mannosidase inhibitor,
- Improved synthetic method
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