The late stage functionalization (LSF) of complex biorelevant compounds is a powerful tool to speed up the identification of structure-activity relationships (SARs) and to optimize ADME profiles. To this end, visible-light photocatalysis offers unique opportunities to achieve smooth and clean functionalization of drugs by unlocking site-specific reactivities under generally mild reaction conditions. This review offers a critical assessment of current literature, pointing out the recent developments in the field while emphasizing the expected future progress and potential applications. Along with paragraphs discussing the visible-light photocatalytic synthetic protocols so far available for LSF of drugs and drug candidates, useful and readily accessible synoptic tables of such transformations, divided by functional groups, will be provided, thus enabling a useful, fast, and easy reference to them.

Visible light photocatalysis in the late-stage functionalization of pharmaceutically relevant compounds.

BI-OAc-Accelerated C3–H Alkylation of Quinoxalin-2(1H)‑ones under Visible-Light Irradiation

Recent advances in visible-light-mediated organic transformations in water

Visible-light-induced three-component reaction of quinoxalin-2(1H)-ones, alkenes and CF3SO2Na leading to 3-trifluoroalkylated quinoxalin-2(1H)-ones

Photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones

Photoredox Catalyst Free, Visible Light‐Promoted C3−H Acylation of Quinoxalin‐2(1 H )‐ones in Water

Divergent Synthesis of Aziridine and Imidazolidine Frameworks under Blue LED Irradiation.

A blue-light-emitting diode (LED) promoted coupling of aryl diazoacetates with sulfur ylides is described. This protocol features mild conditions, good functional group tolerance, and broad substrate scope for both aryl diazoacetates with sulfur ylides. Under optimal reaction conditions, a wide range of trisubstituted olefins is obtained in moderate to good yield, which can be further transferred to other biologically important heterocycles after a two-step simple operation.

Juan Lu

Papers

BI-OAc-Accelerated C3–H Alkylation of Quinoxalin-2(1H)‑ones under Visible-Light Irradiation

Photoredox Catalyst Free, Visible Light‐Promoted C3−H Acylation of Quinoxalin‐2(1 H )‐ones in Water

Divergent Synthesis of Aziridine and Imidazolidine Frameworks under Blue LED Irradiation.

Visible-Light-Promoted Polysubstituted Olefins Synthesis Involving Sulfur Ylides as Carbene Trapping Reagents

Visible Light-Promoted Sulfoxonium Ylides Synthesis from Aryl Diazoacetates and Sulfoxides