化学
产量(工程)
催化作用
对映选择合成
组合化学
磷酸
反应条件
芳基
范围(计算机科学)
有机催化
有机化学
计算机科学
冶金
材料科学
程序设计语言
烷基
作者
Xi Gao,Chengwen Li,Li Chen,Xin Li
出处
期刊:Organic Letters
[American Chemical Society]
日期:2023-10-16
卷期号:25 (42): 7628-7632
标识
DOI:10.1021/acs.orglett.3c02694
摘要
Herein, a highly enantioselective arylation reaction of 3-aryl-5-aminopyrazoles and quinone derivatives was realized using a chiral phosphoric acid catalyst under mild conditions. The reaction has a broad scope with respect to both arylation reaction partners and hence offers rapid access to an array of axially chiral arylpyrazoles with pretty outcomes (up to 95% yield and 99% ee). Notably, the reaction is very efficient, as the catalyst loadings for the model reaction can be reduced to 1 mol % and the enantioselectivity is still maintained. Besides, the synthetic utility of the protocol was proven by a gram-scale reaction and the transformation of the product.
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