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Rh(III)-Catalyzed C–H Activation and [4+1+1] Sequential Cyclization Cascade to Give Highly Fused Indano[1,2-b]azirines
Organic Letters ( IF 5.2 ) Pub Date : 2022-08-03 , DOI: 10.1021/acs.orglett.2c02070
Fuqiang Zheng 1, 2 , Jianhui Zhou 2 , Feifei Fang 2 , Jiyuan Li 2 , Jing Wang 2 , Miao Zheng 2 , Hong Liu 1, 2, 3 , Yungen Xu 1 , Yu Zhou 2, 3
Affiliation  

A Rh(III)-catalyzed C–H activation of α-keto oximes and a cyclization cascade with diazo compounds were developed to construct the highly fused indano[1,2-b]azirine frameworks in good yields with a broad range of substrates under mild reaction conditions. More intriguingly, a [4+1+1] sequential annulation cascade is demonstrated for the first time in this reaction and opened a new reaction mode for α-keto oximes. These fused indano[1,2-b]azirine derivatives could also be further transformed into intriguing privileged drug scaffolds.

中文翻译:

Rh(III)-催化的 C-H 活化和 [4+1+1] 顺序环化级联得到高度融合的茚满并[1,2-b]氮杂环丙烷

开发了 Rh(III) 催化的 α-酮肟的 C-H 活化和与重氮化合物的环化级联反应,以良好的产率构建高度稠合的茚满并[1,2- b ] 氮杂环丙烷骨架,并具有广泛的底物范围反应条件温和。更有趣的是,在该反应中首次证明了[4+1+1]顺序环化级联反应,并为α-酮肟开辟了新的反应模式。这些融合的茚满并[1,2- b ]氮丙啶衍生物也可以进一步转化为有趣的特权药物支架。
更新日期:2022-08-03
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