Diastereoselective Copper-Mediated Conjugate Addition of Functionalized Magnesiates for the Preparation of Bisaryl Nrf2 Activators.
J Org Chem
; 86(4): 3120-3137, 2021 Feb 19.
Article
em En
| MEDLINE
| ID: mdl-33555189
ABSTRACT
A two-step metal-halogen exchange and diastereoselective copper-mediated Michael addition onto a complex α,ß-unsaturated system has been developed and applied toward the synthesis of bisaryl Nrf2 activators. Optimization of metal-halogen exchange using (n-Bu)3MgLi allowed for the preparation of custom aryl-functionalized magnesiate reagents at noncryogenic temperatures. Following transmetalation, these reagents were used in highly diastereoselective Michael addition reactions.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article