1.
J Org Chem
; 87(10): 6918-6926, 2022 05 20.
Artigo
em Inglês
| MEDLINE
| ID: mdl-35443775
RESUMO
The Mukaiyama-aldol reaction is probably one of the most efficient strategies to prepare synthetically useful ß-hydroxy carbonyl compounds. However, only several reported methods were concerned with the accesses to α-fluoro-ß-hydroxy esters. Herein, we report a protocol for a fluoride anion-mediated Mukaiyama aldol reaction with low catalytic loading in a short reaction time to incorporate fluorine at the α position into ß-hydroxy esters. The method shows good functional-group tolerance and scale-up potential, moreover, is applicable to the late-stage modification of natural products and small molecular drugs.