Recent Advances of the Catalysis Systems in the α-C(sp3) -H Functionalization of Glycine Derivatives

alpha-Amino acids are essential components of proteins, which are not only widely used in biologically active compound syntheses, medicinal chemistry, and the materials industry, but also are useful as organic catalysts or ligands for asymmetric synthesis. Glycines are the most fundamental and sole achiral alpha-amino acids, and are particularly useful building blocks in organic synthesis. Direct alpha-C(sp(3))-H functionalization of glycine derivatives or peptides to construct unnatural alpha-amino acids or peptides has attracted tremendous attention of many scholars in recent decades. The research progress of the alpha-C(sp(3))-H functionalization of glycine derivatives is reviewed during the past five years. The catalysis systems are systematically discussed, and the challenges and opportunities of this field are included.