Simplifying Access to Targeted Protein Degraders via Nickel Electrocatalytic Cross-Coupling.
Angew Chem Int Ed Engl
; 63(16): e202319856, 2024 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-38354272
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.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Níquel
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article