학술논문

Simplifying Access to Targeted Protein Degraders via Nickel Electrocatalytic Cross‐Coupling.
Document Type
Article
Source
Angewandte Chemie International Edition. Apr2024, Vol. 63 Issue 16, p1-5. 5p.
Subject
*NICKEL
*FUNCTIONAL groups
*PROTEINS
*RADICALS (Chemistry)
Language
ISSN
1433-7851
Abstract
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 α‐bromoglutarimide 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, multi‐step 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. [ABSTRACT FROM AUTHOR]