碳酸铯催化吡唑与α,β-不饱和酮的氮杂Michael反应
收稿日期: 2014-06-30
修回日期: 2014-09-24
网络出版日期: 2014-10-09
基金资助
国家自然科学基金(Nos. 21362034, 21162026)、高等学校博士学科点专项科研基金(No. 20136203120005)、甘肃省自然科学基金(No. 1107RJZ189)、西北师范大学青年教师科研能力提升计划(No. NWNU-LKQN-11-15)和甘肃农业大学科技创新基金(No. GAU-CX1115)资助项目.
Cesium Carbonate Catalyzed Aza-Michael Addition of Pyrazole to α,β-Unsaturated Ketones
Received date: 2014-06-30
Revised date: 2014-09-24
Online published: 2014-10-09
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21362034, 21162026), the Research Fund for the Doctoral Program of Higher Education of China (No. 20136203120005), the Provincial Natural Science Foundation of Gansu Province (No. 1107RJZ189), the Program for Improving Scientific Research Ability of Young Teachers of Northwest Normal University (No. NWNU-LKQN-11-15) and the Science and Technology Innovation Fund of Gansu Agricultural University (No. GAU-CX1115).
杨靖亚 , 马奔 , 周红艳 , 占宝华 , 李政 . 碳酸铯催化吡唑与α,β-不饱和酮的氮杂Michael反应[J]. 有机化学, 2015 , 35(1) : 121 -128 . DOI: 10.6023/cjoc201406051
A Cs2CO3-catalyzed aza-Michael reaction of pyrazole to α,β-unsaturated ketones has been developed. With 5 mol% Cs2CO3 as catalyst, a series of β-N1-pyrazoly ketones were achieved in 86%～95% yields after 7～12 h in refluxing dioxane. Both aromatic and aliphatic α,β-unsaturated ketones as well as methacrylate and nitrostyrene are well tolerated. Broad scope of substrate and easily scale up make this protocol really practical. Furthermore, the product could be facilely transformed into corresponding γ-amino alcohol.
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