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发展了一种苯甲酰胺自由基自由基环化制备α-官能化叔烷基取代的异喹啉二酮的新反应。此环化反应以偶氮试剂为α-取代叔烷基自由基源物质,利用碘化亚铜/空气体系催化N-烷基-N-甲基丙烯酰基苯甲酰胺发生环化,经过串联自由基加成/环化/碳-碳键形成过程,一步构建了三重碳-碳键,以41%~71%的产率合成了一系列异喹啉二酮及其衍生物。特别值得提出得是,此研究发展了一种新型α-官能叔烷基自由基源物质,发现了一种同时引入两个α-官能叔烷基片段的串联新反应。反应底物适应范围广,反应高效,催化体系廉价实用,为具有潜在药用价值的含α-取代季碳中心的异喹啉二酮及衍生物的合成提供了一条廉价、简单、快捷的新途径。
A novel reaction of benzamide free radical cyclization to prepare α-functionalized tertiary alkyl substituted isoquinolinediones was developed. This cyclization reaction azo reagent for the α-substituted tertiary alkyl radical source material, the use of cuprous iodide / air system catalyzed N-alkyl-N-methacrylylbenzamide cyclization, through a series of free A series of isoquinolinedione and its derivatives were synthesized in 41% ~ 71% yield by one-step construction of the triple carbon-carbon bond formation, the base addition / cyclization / carbon-carbon bond formation process. Particularly worth mentioning is that this study developed a new α-functional tertiary alkyl free radical source material, found a simultaneous introduction of two α-functional tertiary alkyl fragments of the new series of reactions. The reaction substrate has a wide range of adaptability, high reaction efficiency, low cost and practicality of the catalytic system, and provides a cheap, simple and quick new method for the synthesis of isoquinolinedione and derivatives with α-substituted quaternary carbon centers with potential medicinal value. way.