Affiliation:
1. Institute of Advanced Studies and School of Pharmaceutical Sciences Taizhou University Jiaojiang Zhejiang 318000 People's Republic of China
2. School of Pharmaceutical Science Zhejiang Chinese Medical University Hangzhou 310053 People's Republic of China
3. College of Material Chemistry and Chemical Engineering Key Laboratory of Organosilicon Chemistry and Material Technology Ministry of Education Hangzhou Normal University Hangzhou 311121 People's Republic of China
Abstract
AbstractAn efficient and regioselective cyclization for construction of pyrazolo[3,4‐b]pyridines and methylene‐bridged bis(pyrazolo[1,5‐a]pyrimidines) has been established. It involves a [3+2+1] annulation of 3(5)‐aminopyrazole, N,N‐dimethylethanolamine (DMEA), with 1,2‐insertion of aryl methyl ketones or 2,1‐insertion of aryl alkynes. DMEA is oxidized through C(sp3)‐H activation to provide a single or triple carbon source.