Photocatalyzed Minisci-type reactions for late-stage functionalization of pharmaceutically relevant compounds

The Minisci-type reaction, as a versatile tool in the construction of substituted N-heteroarenes, has evolved rapidly since it was first realized and defined. The last decade has witnessed tremendous advances in Minisci-type reactions due to the advent of photoredox catalysis, reflected both in more abundant radical precursors and mild reaction conditions, which offers new opportunities for the functionalization of complex heteroarene-containing scaffolds. This review mainly focuses on the application of photocatalyzed Minisci-type reactions in the late-stage functionalization (LSF) of drugs and drug candidates, and it also includes mechanistic investigations concerning the generation of diverse radicals, aiming to accelerate the discovery of drug candidates and provide medicinal chemists with a comprehensive toolbox and guidance. The application of photocatalyzed Minisci-type reactions in LSF accelerates the discovery of drug candidates in a green way.