Jiang Zi-Yu, Huang Zhe-Yao, Yang Hong, Zhou Lin, Li Qing-Han, Zhao Zhi-Gang
Key Laboratory of General Chemistry of the National Ethnic Affairs Commission, College of Chemistry and Environment, Southwest Minzu University Chengdu 610041 P. R. China
RSC Adv. 2022 Jul 1;12(30):19265-19269. doi: 10.1039/d2ra02314h. eCollection 2022 Jun 29.
A highly efficient method for the synthesis of azole derivatives a direct aza-Michael addition of azoles to α,β-unsaturated malonates using CsCO as a catalyst, has been successfully developed. A series of azole derivatives have been obtained in up to 94% yield and the reaction could be amplified to gram scale in excellent yield in the presence of 10 mol% of CsCO.
已成功开发出一种高效合成唑类衍生物的方法——使用碳酸铯作为催化剂，使唑类与α,β-不饱和丙二酸酯直接进行氮杂迈克尔加成反应。已获得了一系列唑类衍生物，产率高达94%，并且在10 mol%碳酸铯存在下，该反应可以放大至克级规模，且产率优异。
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