Rapid Ti(Oi-Pr)4 facilitated synthesis of α,α,α-trisubstituted primary amines by the addition of Grignard reagents to nitriles under microwave heating conditions
作者:Ruifang Wang、Brian T. Gregg、Wei Zhang、Kathryn C. Golden、John F. Quinn、Peng Cui、Dmytro O. Tymoshenko
DOI:10.1016/j.tetlet.2009.09.178
日期:2009.12
A series of carbinamines (α,α,α-trisubstituted amines) have been prepared in a simple and efficient one-pot procedure by the addition of Grignard reagents to a series of aliphatic, aromatic and heteroaromatic nitriles. The resulting magnesium imines are subsequently converted to the desired amine after treatment with Ti(Oi-Pr)4 and additional microwave heating. Key to this procedure is the use of microwave
通过将格氏试剂添加到一系列脂族,芳族和杂芳族腈中,以简单有效的一锅法制备了一系列卡宾胺(α,α,α-三取代胺)。在用Ti(O i -Pr)4处理和另外的微波加热之后,将得到的镁亚胺随后转化为所需的胺。该程序的关键是在反应方案的两个步骤中都使用了微波加热,这显着提高了两个反应的收率并缩短了反应时间。通常,格利雅(Grignard)加成反应在100°C下5-10分钟内完成,然后用Ti(O i -Pr)4转化,再进行微波加热,以高收率得到目标胺。