通过3+2循环添加基化物合成进入多功能分子
Franz-Lucas Haut1, Christoph Habiger1, Klaus Speck2
1Institute of Organic Chemistry and Center for Molecular Biosciences, Leopold-Franzens-University Innsbruck , Innrain 80-82 , 6020 Innsbruck , Austria.
Journal of the American Chemical Society
|August 14, 2019
概括
这项研究探讨了使用基化物进行 [3+2] 循环添加反应,从而产生多用途的基衍生物. 高压条件提高了具有挑战性的基质的产量,并使药物合成成为可能.
科学领域:
- 有机化学
- 合成化学
- 医学化学
背景情况:
- 硫化物是反应性的中间体.
- 循环添加反应是关键的合成工具.
- 获得复杂的含硫异环是有价值的.
研究的目的:
- 调查基和基的二氧化碳化物 [3+2] 循环添加.
- 开发多用途的合成途径,使烯衍生物.
- 为了证明药物合成的实用性.
主要方法:
- [3+2]-循环添加反应
- 使用高压条件.
- 二和四基中间体的合成.
主要成果:
- 与多种基和基成功循环添加.
- 形成多用途的二和四基产物.
- 在高压下提高产量达58%.
- 获得类,类,类树和副四元中心.
结论:
- [3+2]-环添加是一种合成硫异环的有效方法.
- 高压条件提高了反应范围和效率.
- 这种方法为药物发现提供了有价值的中间体,包括NGB 4420和tenilapine.
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