一种化学酶方法,用于制备具有高光学产量的埃菲纳可纳
Zhiran Ju1, Zhiyun Li1, Menglan Li1
1Institute of Pharmaceutical Science and Technology, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China.
The Journal of organic chemistry
|October 4, 2023
概括
我们开发了一种绿色生物催化方法,使用甲酶 (BAL) 合成抗真菌药物efinaconazole. 这种环保的工艺在生产这种重要的抗真菌剂方面比传统的化学合成具有优势.
科学领域:
- 生物催化剂是一种生物催化剂.
- 有机合成 有机合成
- 药用化学 医学化学
背景情况:
- 埃菲纳可纳是一种关键的抗真菌剂.
- 传统的合成方法可能对环境造成负担.
- 在制药制造业中,更绿色的合成路径非常理想.
研究的目的:
- 开发一种环保的生物催化方法来合成efinaconazole.
- 为了利用甲酶 (BAL) 作为关键的合成步骤.
- 建立一个高效和可扩展的生产过程.
主要方法:
- 使用甲酶 (BAL) 催化子凝.
- 作为基质使用了2,4-二二甲.
- 作为辅助因子,加入了胺二酸盐 (ThDP) 和Mg2+.
主要成果:
- 通过生物催化成功合成了α-基的前体.
- 开发了一种新的途径到efinaconazole (7).
- 对于efinaconazole,获得了38%的中等整体产量.
结论:
- 生物催化方法为化学合成提供了一个更绿色的替代方案.
- 这种方法比传统的化学工艺具有显著的优势.
- 建立了有效和可扩展的程序,以生产efinaconazole.
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