诺福维尔的化学酶合成
Beata Zdun1, Tamara Reiter2, Wolfgang Kroutil2
1Laboratory of Biocatalysis and Biotransformation, Department of Drugs Technology and Biotechnology, Faculty of Chemistry, Warsaw University of Technology, Koszykowa 75, 00-662 Warsaw, Poland.
The Journal of organic chemistry
|July 19, 2023
概括
用于特诺福维尔合成的新型化学酶方法利用了具有成本效益的初始材料和酶. 这些途径使关键中间体的高效生产成为可能,为特诺福维尔及其衍生物TDF和TAF铺平了道路.
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:
- 诺福维尔是一种重要的抗病毒药物.
- 需要有效且具有成本效益的合成途径.
- 化学酶方法提供了可持续的替代方案.
研究的目的:
- 为特诺福维尔病毒开发新的化学酶合成途径.
- 为了利用低成本的原料和酶生物催化剂.
- 探索关键中间体的立体选择性酶化步骤.
主要方法:
- 使用固定脂酶用于以介质的动力分辨率.
- 使用酒精脱酶 (ADH) 进行基的立体选择性降解.
- 执行"一"反应进行中间转化和最终产品合成.
主要成果:
- 使用脂酶获得了 (R) 的99%的效应.
- 使用ADH获得>99% ee和 (R) - 酒精的86%产量.
- 成功合成了tenofovir,并证明了对TDF和TAF衍生物的适用性.
结论:
- 开发了用于特诺福维尔合成的高效化学酶路径.
- 酶策略可用于生产特诺福维尔及其前药物.
- 分子对接提供了对酶立体选择性的见解.
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