基的催化二重选择性和选择性胺
Katrina M Mennie1, Steven M Banik1, Elaine C Reichert1
1Department of Chemistry & Chemical Biology , Harvard University , Cambridge , Massachusetts 02138 , United States.
Journal of the American Chemical Society
|March 28, 2018
概括
这项研究报告了一种使用催化剂合成化基的新方法. 这种方法为药物发现提供了对有价值的有机化合物的高度选择性访问.
科学领域:
- 有机化学
- 不对称的合成
- 化化学
背景情况:
- 化物有机化合物是药物化学的重要组成部分.
- 开发高效和刻板选择的合成方法仍然是一个重大挑战.
研究的目的:
- 开发一种新型的催化系统,用于合成β-化衍生物.
- 探索这种方法对其他具有多个立体中心的化化合物的实用性.
主要方法:
- 使用HF-pyridine和mCPBA催化化化胺.
- 使用催化剂控制的二重选择性来合成复杂的胺.
- 开发方法应用于各种基质.
主要成果:
- 在syn-β-fluoroaziridines的合成中具有很高的二重选择性和反选择性.
- 用三个连续立体中心成功制备富含的1,3-二胺.
- 获得来自不同基质的抗β-甲和1,2-氧化产品.
结论:
- 开发的化酸催化剂能够有效地对有价值的化有机构件进行立体选择性合成.
- 该方法可用于访问具有多个立体中心的复杂化分子.
- 这项工作为合成化药物和农业化学品提供了强大的工具.
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