Bioorthogonal Ligations and Cleavages in Chemical Biology

Abstract Bioorthogonal reactions including the bioorthogonal ligations and cleavages have become an active field of research in chemical biology, and they play important roles in chemical modification and functional regulation of biomolecules. This review summarizes the developments and applications of the representative bioorthogonal reactions including the Staudinger reactions, the metal‐mediated bioorthogonal reactions, the strain‐promoted cycloadditions, the inverse electron demand Diels‐Alder reactions, the light‐triggered bioorthogonal reactions, and the reactions of chloroquinoxalines and ortho ‐dithiophenols.