Oxaziridine-Mediated Amination of Primary Amines: Scope and Application to a One-Pot Pyrazole Synthesis
作者:Alan Armstrong、Lyn H. Jones、Jamie D. Knight、Richard D. Kelsey
DOI:10.1021/ol0474507
日期:2005.2.1
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. [Reaction: see text]
据报道,使用二乙基酮戊二酸酯衍生的恶唑烷进行伯脂族胺和芳族胺的亲电胺化反应,以良好或优异的收率得到相应的N-Boc肼。该方法允许从伯胺一锅法合成吡唑。[反应:请参阅文字]