用In Situ生成的HOCl作为键来源的N-替代胺的催化酶选择性功能化
Tengbo Ding1, Liang Long2, Mei-Jie Yuan1
1State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, China.
这项研究引入了一种新的催化方法,用于从没有键供体的氨基胺中制造性环. 该过程有效合成具有高反选择性的复杂氧丁和氨基.
科学领域:
- 有机化学
- 不对称的催化
- 合成方法
背景情况:
- 不对称的有机催化环化对于性环合成至关重要.
- 目前的方法很大程度上依赖于具有键捐赠者的基板,限制了应用.
- 需要更广泛的基质范围在enantioselective halocyclization.
研究的目的:
- 开发一种缺乏键供体的胺的催化不对称功能化.
- 通过四元立体中心有效地产生性氧-2-和氨基.
- 为合成N-aryloxazolidin-2-ones和抗生素类似物建立一个多功能框架.
主要方法:
- 使用新型有机催化系统的催化不对称功能化.
- 用各种胺基进行基质范围探索.
- 在现场产生HOCl的机械研究.
主要成果:
- 获得了高产量和优异的氧-2-和氨基.
- 有关抗生素结构的N-aryloxazolidin-2-ones的成功合成.
- 确定水在化剂激活中的关键作用.
结论:
- 已经建立了一个强大的催化系统,用于非激活的氨基胺的不对称功能化.
- 开发的方法克服了以前依赖键供体的策略的局限性.
- 这项工作扩大了环化用于创建多样化,丰富分子的实用性.
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