School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Ajmer, Rajasthan 305817, India.
Chem Commun (Camb). 2020 Apr 30;56(35):4804-4807. doi: 10.1039/d0cc00826e.
Herein, we report a highly facile and unprecedented approach to synthesize congested N-(hetero)aryl amines en route to α-amino acid amides using α-bromoamides as alkylating agents under mild reaction conditions (room temperature). The involvement of aza-oxyallyl cations as alkylating agents is the hallmark of this reaction. The method was readily adapted for the rapid synthesis of coveted 1,4-benzodiazepine-3,5-diones.
在此,我们报告了一种非常简便且前所未有的方法,即在温和的反应条件(室温)下,使用α-溴酰胺作为烷基化试剂,合成拥挤的 N-(杂)芳基胺,进而合成α-氨基酸酰胺。该反应的特点是使用氮杂氧杂烯阳离子作为烷基化试剂。该方法很容易适应于令人垂涎的 1,4-苯并二氮杂-3,5-二酮的快速合成。