催化降解回收功能化异佐N-氧化物到罗利丁-3-one
Ilya V Okladnikov1,2, Svetlana A Aksenova3,4, Sema L Ioffe1
1N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky prospect, 47, 119991 Moscow, Russian Federation.
The Journal of organic chemistry
|December 14, 2023
概括
一种新方法从异素N-氧化物中合成了多替代的pyrrolizidine-3-one. 这种催化降解多米诺过程是二分体选择性的,产生用于制药应用的特定异构体.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 合成化学 合成化学
背景情况:
- 罗利丁是天然产品和制药中的一个关键支架.
- 对于pyrrolizidines而言,现有的合成途径可能很复杂.
- 需要新的策略来高效的合成pyrrolizidine.
研究的目的:
- 开发一种新的催化还原型多米诺型回收利用策略.
- 为了高效地合成多替代的pyrrolizidine-3-ones.
- 为了探索开发的合成路线的立体选择性.
主要方法:
- 催化还原型多米诺型回收利用.
- 伊索克萨林N-氧化物的功能化.
- 灾难选择性合成.
主要成果:
- 建立了用于pyrrolizidine-3-ones的新合成策略.
- 该过程显示出高的二聚体选择性,有利于一种同位素.
- 合成了修改后的GSK的PDE4抑制剂和MSD的hNK1抗剂.
结论:
- 开发的方法提供了高效的访问多替代的pyrrolizidine-3-ones.
- 合成的散列选择性是药物开发的优势.
- 这种方法可以制备已知的制药剂的新型类似物.
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