Simplifying Access to Targeted Protein Degraders via Nickel Electrocatalytic Cross‐Coupling

Author:

Neigenfind Philipp1,Massaro Luca12,Péter Áron1,Degnan Andrew P.3,Emmanuel Megan A.4,Oderinde Martins S.3,He Chi5,Peters David5,El‐Hayek Ewing Tamara1,Kawamata Yu1,Baran Phil S.1ORCID

Affiliation:

1. Department of Chemistry Scripps Research 10550 North Torrey Pines Road 92037 La Jolla CA United States

2. Department of Chemistry KTH Royal Institute of Technology Teknikringen 30 S-10044 Stockholm Sweden

3. Small Molecule Drug Discovery Bristol Myers Squibb Research & Early Development Route 206 & Province Line Road 08543 Princeton NJ United States

4. Chemical Process Development Bristol Myers Squibb 1 Squibb Drive 08901 New Brunswick NJ, United States

5. Small Molecule Drug Discovery Bristol Myers Squibb Research & Early Development 10300 Campus Point Drive 92121 San Diego CA United States.

Abstract

AbstractC−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.

Funder

NSF Center for Synthetic Organic Electrochemistry, University of Utah

Publisher

Wiley

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