CIBION   24492
CENTRO DE INVESTIGACIONES EN BIONANOCIENCIAS "ELIZABETH JARES ERIJMAN"
Unidad Ejecutora - UE
artículos
Título:
Mechanism-Based Solution to the ProTide Synthesis Problem: Selective Access to Sofosbuvir, Acelarin, and INX-08189
Autor/es:
LIU, ZHUQING; SILVERMAN, STEVEN M.; SIMMONS, BRYON; BELLOMO, ANA; KLAPARS, ARTIS
Revista:
ORGANIC LETTERS
Editorial:
AMER CHEMICAL SOC
Referencias:
Año: 2017
ISSN:
1523-7060
Resumen:
A general and efficient method for the synthesis of pronucleotide (ProTide) 5?-phosphoramidate monoesters is reported. This method consists of a highly stereoselective 5?-phosphorylation mediated by dimethylaluminum chloride to afford the desired target ProTides in excellent yields withoutemploying 3?-protection strategies. The application of this methodology to the synthesis of a number of pharmaceutically relevant compounds currently marketed or under investigation in clinical research is demonstrated.