Direct amination of pyrimidin-2-yl tosylates with aqueous ammonia under metal-free and mild conditions

A metal-free synthesis of pyrimidine functionalized primary amines via direct amination of pyrimidin-2-yl tosylate with aqueous ammonia has been developed under mild conditions. The desired products pyrimidin-2-amines can be generated in excellent yields in PEG-400, without any catalysts or other additives.

Graphical abstractA metal-free synthesis of pyrimidine functionalized primary amines via direct amination of pyrimidin-2-yl tosylates with aqueous ammonia under mild conditions was developed.Figure optionsDownload full-size imageDownload as PowerPoint slide