循环二次氨基的氧化脱动态分辨率
Ran Lu1, Liya Cao1, Honghao Guan2
1School of Pharmaceutical Sciences , Shandong University , Jinan 250012 , China.
Journal of the American Chemical Society
|March 28, 2019
概括
一种新的铁催化方法使用空气实现了循环二次胺的有效动态分辨率. 这种实用方法产生了基丰富的氨基,包括复杂的生物活性分子中间体.
科学领域:
- 有机化学
- 催化剂
- 不对称的合成
背景情况:
- 动态分辨率对于获得质纯化合物至关重要.
- 开发有效和可持续的氨基合成催化方法是一个持续的挑战.
研究的目的:
- 报告循环二次胺的非酶化,铁催化脱动态分辨率.
- 建立一种经济和实用的方法来获取基丰富的循环氨基.
主要方法:
- 使用非酶铁催化剂进行脱水动力分辨.
- 使用空气作为可持续的氧化剂.
- 将该方法应用于各种循环胺,包括5,6-二二丁和1,2-二基诺林.
主要成果:
- 对一系列循环二次氨基的高产量和优秀的反选择性.
- 对具有多种α位置功能组的基板的证明适用性.
- 通过其他不对称的方法来合成具有挑战性的生物活性分子的先进中间体.
结论:
- 开发的铁催化方法为循环二次胺的不对称合成提供了一种高效,经济和实用的途径.
- 这一战略为药物发现和开发提供了有价值的中间体.
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