铜催化不对称的减少合维尼尔N-异质与Para-基甲基
Bo Chen1,2, Qi-Qiong Yang1, Xiang Zhen1
1State Key Laboratory of Natural Product Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, 222 Tianshui Nanlu, Lanzhou 730000, China.
研究人员开发了一种铜催化方法,以制造性1,1,2-三烯. 这种策略有效地将乙烯基N-异二烯与基甲基结合,产生用于药物化学的有价值化合物.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 不对称的合成方法
背景情况:
- 的1,1,2-三乙烯是药物发现中的重要组成部分.
- 现有的合成方法可能缺乏效率或立体控制.
研究的目的:
- 开发一种新的铜催化不对称的还原性合策略.
- 为了合成含有N- heteroarene部分的奇拉性1,1,2-三亚利乙烯.
主要方法:
- 乙烯基N-异质与帕拉基甲基 (p-QM) 的合.
- 使用铜催化剂进行不对称的诱导.
- 针对产量和立体选择性的反应条件的优化.
主要成果:
- 取得的收益率在60-99%之间.
- 获得高选择性,高达94% ee.
- 从2:1到>20:1的时间表中表现出良好的 diastereoselectivities.
结论:
- 开发的协议提供了一个模块化和高效的途径,以奇拉的triarylethanes.
- 该方法采用低成本的催化剂和易于获得的基板.
- 提供对立体选择性的优良控制,对药物化学应用有价值.
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