酰胺类杂环烯酮缩胺的合成
收稿日期: 2016-07-02
修回日期: 2016-08-25
网络出版日期: 2016-09-08
基金资助
国家自然科学基金(Nos. 21362042,U1202221,21662042)、云南省后备人才(No. 2012HB001)、云南大学青年英才计划(No. XT412003)资助项目.
Synthesis of Amide Class Heterocyclic Ketene Aminals
Received date: 2016-07-02
Revised date: 2016-08-25
Online published: 2016-09-08
Supported by
Project supported by the National Natural Science Foundation of China(Nos. 21362042, U1202221, 21662042), the Talent Found in Yunnan Province(No. 2012HB001), and the Excellent Young Talents, Yunnan University(No. XT412003).
罗大云 , 崔时胜 , 胡兴梅 , 林军 , 严胜骄 . 酰胺类杂环烯酮缩胺的合成[J]. 有机化学, 2017 , 37(1) : 166 -175 . DOI: 10.6023/cjoc201607002
In this paper,a concise protocol for synthesis of possess potential pharmacological active amide class heterocyclic ketene aminals(HKAs) has been developed,which based on the six or seven-membered HKAs 1~2,using aryl isocyanate 4 as acylation agent.The regioselective acylation reaction of HKAs in 1,4-dioxane at room temperature gave compounds 5~6 with 90%~98% yields.However,the five-membered HKAs 3 and aryl isocyanate 4 reacted in 1,4-dioxane catalyzed by Cs2CO3 at room temperature to obtain compounds 7 in 78%~93% yields.
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