恩利酸的总合成
Hongming Li1, David A Thaisrivongs1, Gao Shang1
1Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States.
Journal of the American Chemical Society
|March 24, 2025
概括
我们合成了一种新型的口服蛋白转化酶抑制剂, 为了大规模生产这种复杂的,开发了一种强大的制造工艺.
科学领域:
- 医学化学
- 心血管医学
- 过程化学
背景情况:
- 动脉样性心血管疾病 (ASCVD) 是全球主要的死亡原因.
- 蛋白转化酶9型抑制剂 (PCSK9) 是治疗高脂血症和降低心血管风险的一种有前途的治疗策略.
- 恩利酸是一种正在开发的口服PCSK9抑制剂,用于ASCVD治疗.
研究的目的:
- 报告化的总合成.
- 描述大型化物生产制造工艺的发展.
主要方法:
- 融合合成的战略.
- 开发一个强大而高效的制造工艺.
- 合成的酸的特征.
主要成果:
- 已经成功合成了酸.
- 建立一个可扩展的制造工艺.
- 恩利酸是一种复杂的宏环,具有非的结构元素.
结论:
- 开发的合成和制造工艺可以大规模生产酸.
- 这项研究有助于临床开发用于动脉样硬化心血管疾病的恩利西.
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