埃纳提选择性迈克尔添加到阿尔法,β不和胺基,由盐-Al复合物催化
Mark S Taylor1, Eric N Jacobsen
1Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA.
Journal of the American Chemical Society
|October 14, 2005
概括
一种新型的 () 复合物有效催化并联加法反应,产生有价值的多功能化合物. 这种方法可实现对比的合成对比性丰富的piperidines,包括一条通往 (-) -paroxetine的路径.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 不对称的合成方法
背景情况:
- 结合物加法反应对于C-C键的形成至关重要.
- 获取富含的多功能化合物仍然是一个合成挑战.
研究的目的:
- 开发一种高效的催化系统,用于合添加化.
- 为了合成新的富含的多功能化合物.
- 为了证明在制药中间制剂中的合成应用.
主要方法:
- 使用 (沙伦) 复合物作为催化剂.
- 对α,β不和 imides 进行二和三替代烯的结合添加.
- 应用产品在非对称合成的piperidines.
主要成果:
- (Salen) 复合物表现出高的催化效率.
- 一种广泛的非循环基和基替代因化物被成功地功能化.
- 合成了富含酵素的piperidines,包括一个通往 (-) -paroxetine的途径.
结论:
- 已经建立了一种新的方法来进行非对称的合添加化.
- 这种方法可以获得以前无法获得的丰富多功能化合物.
- 该方法适用于合成有价值的制药构建块.
相关概念视频
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Alkenes can be obtained from amines via an E2 elimination. The amine is first converted into a good leaving group, such as a quaternary ammonium salt. This is accomplished by treating the amine with an excess of alkyl halide, which results in a halide salt. Next, the halide salt is transformed into a hydroxide salt that functions as a base to enable elimination.
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