装饰N-氧化物异诺林的合成:在循环反应中的阿里烯酸
João M Anghinoni1, Sabrina S Ferreira1, Jean C Kazmierczak2
1Centro de Ciências Químicas, Farmacêuticas e de Alimentos (CCQFA), Universidade Federal de Pelotas (UFPel), P.O. Box 354, Pelotas, 96010-900 Rio Grande do Sul, Brazil.
The Journal of organic chemistry
|August 1, 2024
概括
酸衍生物 (BSA) 提供了一个稳定的源,用于合成装饰的异类N-氧化物. 这种新方法为新型化合物生成提供了高产量和可扩展性.
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:
- 异类N-氧化物是药物化学中的重要支架.
- 将引入有机分子的高效方法是有价值的.
- 现有的试剂可能不稳定或难以处理.
研究的目的:
- 开发一种用于有机合成的新型稳定试剂.
- 建立一种新协议,用于合成装饰着的异诺林N-氧化物.
- 探索所开发的反应的范围和可扩展性.
主要方法:
- 作为的来源,使用酸衍生物 (BSA).
- 采用了o-alkynyl甲氧化物的环化.
- 在反流甲醇中进行反应,以在现场产生电友的.
主要成果:
- 成功合成了19个装饰着的异素N-氧化物库.
- 达到高达96%的产量,具有出色的基材耐受性.
- 证明了反应的可扩展性是10倍 (0.25到2.5毫摩尔).
结论:
- 酸衍生物 (BSA) 是有效且易于使用的试剂.
- 开发的单环化协议对于获取多种异诺林N-氧化物是有效的.
- 这种方法提供了一条可扩展的途径,以获得含有的新型异环化合物.
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