通过后期阶段不对称转移化合成 (S) - 芬
Zihao Dai1, Jiamu Liu1, Naixing Wang2
1State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200032, China.
Organic letters
|February 27, 2026
概括
开发了一种新合成的 (S) - finerenone,一个矿物质皮质类受体对手. 这种方法为药物提供了一个可扩展,高收益,和enantioselective的工业生产平台.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 过程化学 过程化学
背景情况:
- 菲内伦是一种非类固醇矿物质皮质类受体对抗剂.
- 有效和可扩展的合成对于制药生产至关重要.
研究的目的:
- 开发一种实用且可扩展的 (S) -finerenone合成方法.
- 建立一个灵活,高收益和反选择性的生产平台.
主要方法:
- 融合合成利用一个racemic前体.
- 无染色学可扩展的前体合成方法 (88%的产量).
- 两个互补的方法,以实现对抗选择性分辨率: (+) - 基酸分辨率和非对称的转移化与酸催化动态动态动态分辨率 (DKR).
主要成果:
- 获得了88%的整体产量,用于赛血基前体.
- 开发了可靠和高效的方法来获得纯 (S) - 芬.
- 展示了一个适合工业规模生产的灵活平台.
结论:
- 报告中的合成为 (S) -finerenone提供了一个可行的工业规模生产途径.
- 开发的方法避免了繁的净化,提供了高产量和酶选择性.
- 这种方法提高了关键治疗剂的可访问性.
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