N-Trifluoropropylation of Azoles through N-Vinylation and Sequential Hydrogenation.
J Org Chem
; 87(22): 15703-15712, 2022 11 18.
Article
de En
| MEDLINE
| ID: mdl-36331418
ABSTRACT
Installing a fluoroalkyl group onto the nitrogen atom of azoles represents a potential strategy for lead optimization in medicinal chemistry. Herein, we describe a method for the N-trifluoropropylation of azoles. This process is accomplished using a combination of regioselective N-vinylation and sequential hydrogenation. The two-step sequence is applicable to a diverse set of azoles and tolerates a wide range of functionalities. In addition, we showcase its practicability and utility through the gram-scale synthesis and the late-stage modification of a complex molecule.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Azoles
/
Azote
Langue:
En
Journal:
J Org Chem
Année:
2022
Type de document:
Article