Key Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Provincial Key Laboratory for Research and Development of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, People’s Republic of China
Received: 17 September 2020 Accepted: 9 March 2021
An effective strategy for the chemoselective synthesis of β-enaminones is described by aza-Michael addition of aminoalkyl-, phenol- and thio-anilines to ynones under metal-free conditions. Diverse structural β-enaminones were obtained in up to 99% yield for 31 examples. The novel dual-1,5-disubstituted triazole scaffold was synthesized subsequently from β-enaminone. This strategy is highly efficient, highly chemoselective and metal-free.
Keywords: Chemoselective; β-enaminones; Ynones; Amines with two nucleophilic sites; Metal-free