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Home » total synthesis » Total Synthesis of (−)‐Indoxamycins A and B

Total Synthesis of (−)‐Indoxamycins A and B

Angew. Chem. Int. Ed. 2019, 58, 1 – 5
DOI: 10.1002/anie.201902043  
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文献汇报人:赵志文

汇报日期: 2019413

图文摘要:

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  • 推荐原因:


    梁广鑫教授从廉价易得的R-香芹酮衍生物出发,利用以Pauson-Khand 反应为关键步骤的3步反应快速构建了含甲基季碳手性中心的[5,5,6]三环核心笼状结构,铜催化的1,4-加成构建另一个相邻的含甲基季碳手性中心,然后利用逆氧杂迈克尔加成/1,2-加成/氧杂迈克尔加成串联反应高效引入丁烯基侧链,后期通过1,3-羰基化合物的烷基化实现第三个含甲基季碳手性中心的构筑,最终以13步反应完成了()-indoxamycin A 的全合成。在()-Indoxamycin B的全合成中,他们则通过Mukaiyama aldol 反应构建目标分子个性化的羟甲基季碳中心,最终以总路线16步反应完成其全合成。


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