期刊
ORGANIC LETTERS
卷 22, 期 18, 页码 7135-7140出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c02488
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资金
- Guangzhou University of Chinese Medicine, Pearl River Talents Recruitment Program of Guangdong Province [2017GC010361]
- Department of Education of Guangdong Province [2016KCXTD015]
- Jiangmen Program for I nnovative Research Team [2018630100180019806]
The construction of cyclobutanes has attracted much attention because of its unique four-membered ring skeleton. Herein, we report the highly enantioselective direct vinylogous Michael reaction of beta,gamma-unsaturated pyrazole amides and nitroolefin using a squaramide catalyst. Cyclobutane derivatives were obtained by subsequent cyclization in good yields (up to 85%) with excellent enantioselectivities (up to 99% ee). Importantly, the large-scale reaction experiment confirmed the reliability of the vinylogous reaction. Furthermore, the synthetic utility of the vinylogous adducts and cyclobutane derivatives has been realized.
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