A Buchwald-Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3-Ligase PROTACs*.
PEPPSI
PROTAC
amination
cereblon
drug discovery
Journal
Chemistry (Weinheim an der Bergstrasse, Germany)
ISSN: 1521-3765
Titre abrégé: Chemistry
Pays: Germany
ID NLM: 9513783
Informations de publication
Date de publication:
15 Dec 2020
15 Dec 2020
Historique:
received:
01
07
2020
revised:
22
07
2020
pubmed:
25
7
2020
medline:
20
2
2021
entrez:
25
7
2020
Statut:
ppublish
Résumé
A palladium-catalysed Buchwald-Hartwig amination for lenalidomide-derived aryl bromides was optimised using high throughput experimentation (HTE). The substrate scope of the optimised conditions was evaluated for a range of alkyl- and aryl- amines and functionalised aryl bromides. The methodology allows access to new cereblon-based bifunctional proteolysis targeting chimeras with a reduced step count and improved yields.
Identifiants
pubmed: 32706492
doi: 10.1002/chem.202003137
doi:
Substances chimiques
Amines
0
Bromides
0
Ligands
0
Ubiquitin-Protein Ligases
EC 2.3.2.27
Lenalidomide
F0P408N6V4
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
16818-16823Informations de copyright
© 2020 Wiley-VCH GmbH.
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