TFE-Facilitated Synthesis of Tetrahydropyridino[2,3-d]pyrimidine via Cascade [1,5]-Hydride Transfer/Cyclization

An efficient fluorinated alcohol-driven cascade [1,5]-hydride transfer/cyclization between o-amino pyridyl aldehydes and primary amines has been developed. This unique transformation enabled an array of tetrahydropyridino[2,3-d]pyrimidine construction. Furthermore, the encouraging antifungal activity of Thanatephorus cucumeris was demonstrated by this tetrahydropyridino[2,3-d]pyrimidine core structure.