Simplifying Access to Targeted Protein Degraders via Ni-Electrocatalytic Cross-Coupling

20 December 2023, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


C–C linked glutarimide-containing structures with direct utility in the preparation of cereblon-based degraders (PROTACs, CELMoDs) can be assessed in a single step from inexpensive, commercial -bromoglutaramide through a unique Brønsted-acid assisted Ni-electrocatalytic approach. The reaction tolerates a broad array of functional groups that are historically problematic and can be applied to the simplified synthesis of dozens of known compounds that have only been procured through laborious, wasteful, multistep sequences. The reaction is scalable in both batch and flow and features a trivial procedure wherein the most time-consuming aspect of reaction setup is weighing out the starting materials.


protein degraders
nickel catalysis
radical retro synthesis

Supplementary materials

Supporting information
spectra, optimization, graphical procedural guide, etc.


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