通过阿里三醇环开放和随后的循环化合成醇衍生物
Aleksejs Burcevs1, Armands Sebris1, Irina Novosjolova1
1Institute of Chemistry and Chemical Technology, Faculty of Natural Sciences and Technology, Riga Technical University, P. Valdena Str. 3, LV-1048 Riga, Latvia.
一种新型的无金属合成,从三醇中产生N替代的. 这种两步方法涉及Dimroth重新排列和Wolff循环,提供选择性访问多种类型的内结构.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
背景情况:
- 印衍生物是药物化学和材料科学中的关键支架.
- 有效和选择性的合成路径到功能化的室内空间是非常受欢迎的.
研究的目的:
- 开发一种无金属的两步合成策略,用于N替代的醇.
- 为了实现选择性合成的1H-indoles和1-aryl-1H-indoles.
主要方法:
- 合成始于含有亚利三醇的化合物.
- 步骤1:迪莫斯平衡,挤出,沃尔夫重组和氨基核添加形成N-乙烯-1,1-胺.
- 步骤2:催化中间体的循环,以获得目标1H-indoles.
主要成果:
- 建立了一个强大的无金属合成路径,以获得N替代的英多尔.
- 该方法提供了在C2位置上具有N替代物的indules的访问.
- 选择性形成1H-英多尔或1--1H-英多尔是通过改变N核友来实现的.
结论:
- 开发的两步方法为醇合成提供了一种多功能和高效的途径.
- 这种方法避免使用过渡金属,与绿色化学原则保持一致.
- 在化步骤中观察到的选择性增强了这种合成策略的实用性.
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