Facile preparation of protected benzylic and heteroarylmethyl amines via room temperature Curtius rearrangement
作者:Matthew L. Leathen、Emily A. Peterson
DOI:10.1016/j.tetlet.2010.03.101
日期:2010.5
Curtius rearrangement of phenyl and heteroaryl acetic acids is described. We have developed a protocol for room temperature Curtius rearrangement in MeOH or CHCl3 that provides an improvement over standard conditions, avoiding the use of additives or heat. This room temperature optimization of the Curtius rearrangement prevents the formation of side products often observed with benzylic acids, allowing
描述了用于形成酰基叠氮化物以及随后的苯基和杂芳基乙酸的Curtius重排的分步室温过程。我们已经开发出了在MeOH或CHCl 3中进行室温Curtius重排的规程,该规程比标准条件有所改进,避免了使用添加剂或加热。Curtius重排的这种室温优化可防止形成通常在苯甲酸中观察到的副产物,从而可以使用各种苯甲基和杂芳基甲基胺。