4.8 Article

Asymmetric Aziridination of Cyclic Enones Using Chiral Diamine Catalysts and Its Application to the Total Synthesis of (-)-Agelastatin A

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ORGANIC LETTERS
卷 13, 期 21, 页码 5744-5747

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AMER CHEMICAL SOC
DOI: 10.1021/ol2023054

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  1. Ministry of Education, Culture, Sports, Science and Technology, Japan
  2. Grants-in-Aid for Scientific Research [23390003, 22790006] Funding Source: KAKEN

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The asymmetric aziridination of cyclic enones with N-tosyloxycarbamates, using N-neopentyl 1,2-diphenylethylenediamine as a catalyst, and its application to the formal total synthesis of (-)-agelastatin A, using a one-pot silylation-selenylation procedure and the regioselective aziridine-opening by an azide anion as key steps, are described.

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