C-H Bond Functionalization of Tetrahydropyridopyrimidines and Other Related Hetereocycles

A novel and efficient 2-step method for the functionalization of the C-H bond adjacent to the amino group of tetrahydropyridopyrimidine (THPP) is reported herein. The reaction features mild conditions and excellent tolerance of a wide range of functional groups. Moreover, this method is applicable to tetrahydroisoquinolone (THIQ), which provides a useful supplement to literature method. This method gives chemists a new tool to functionalize a C-H bond at late stage and may find applications in both synthetic organic and medicinal chemistry.