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.