Creaflow is pleased to share a new peer reviewed article in ChemCatChem. The work explores photoredox strategies to build PROTAC linkers from cereblon ligands. The publisher page is available via the link below.

Method and scope

The study reports a visible light driven reductive cross-coupling that forges C(sp3)-C(sp2) bonds from cereblon based substrates and aryl partners. The authors outline reaction conditions that are broadly applicable, enabling late stage diversification of CRBN warheads for linker exploration. Substrate scope and key parameters are discussed to support reliable use in development settings.

Batch and flow implementation

Beyond batch conditions, the methodology is translated to continuous flow to improve control over irradiation, residence time, and heat management. This provides a practical route for scalable library synthesis and faster iteration during PROTAC design.

Christian O. Kappe et al. “Photoredox Csp3-Csp2 Reductive Cross-Couplings of Cereblon Ligands for PROTAC Linker Exploration in Batch and Flow.” ChemCatChem, 2022. doi: 10.1002/cctc.202201184.