Oxaziridine-mediated amination of primary amines: Scope and application to a one-pot pyrazole synthesis

被引:92
作者
Armstrong, A [1 ]
Jones, LH
Knight, JD
Kelsey, RD
机构
[1] Univ London Imperial Coll Sci Technol & Med, Dept Chem, London SW7 2AZ, England
[2] Pfizer Global R&D, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England
关键词
D O I
10.1021/ol0474507
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] Electrophilic amination of primary aliphatic and aromatic amines is reported using a diethylketomalonate-derived oxaziridine to afford the corresponding N-Boc hydrazines in good to excellent yields. The method allows a one-pot synthesis of pyrazoles from primary amines.
引用
收藏
页码:713 / 716
页数:4
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