Unexpected and Expeditious Entry into Trifluoromethyl Aziridines from Substituted β-Dicarbonyl Compounds
作者:Daniele Colantoni、Stefania Fioravanti、Lucio Pellacani、Paolo A. Tardella
DOI:10.1021/jo0515327
日期:2005.11.1
One-pot aziridinations were obtained starting from substituted 2,2,2-trifluoroethyl β-dicarbonyl compounds with nosyloxycarbamates in the presence of an excess of CaO as base. The unexpected ring closure reaction takes place at room temperature, leading to the N-protected α-trifluoromethyl aziridines with good yields. The reaction pathway seems to be influenced by the choice of the base.
在存在过量的CaO作为碱的情况下,从用壬基氧基氨基甲酸酯取代的2,2,2-三氟乙基β-二羰基化合物开始,进行一锅叠氮化。意外的闭环反应在室温下发生,从而以良好的收率得到N-保护的α-三氟甲基氮丙啶。反应途径似乎受到碱基选择的影响。