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Mechanism-Based Solution to the ProTide Synthesis Problem: Selective Access to Sofosbuvir, Acelarin, and INX-08189
Fecha
2017-05Registro en:
Simmons, Bryon; Liu, Zhuqing; Klapars, Artis; Bellomo Peraza, Ana Ines; Silverman, Steven M.; Mechanism-Based Solution to the ProTide Synthesis Problem: Selective Access to Sofosbuvir, Acelarin, and INX-08189; American Chemical Society; Organic Letters; 19; 9; 5-2017; 2218-2221
1523-7060
CONICET Digital
CONICET
Autor
Simmons, Bryon
Liu, Zhuqing
Klapars, Artis
Bellomo Peraza, Ana Ines
Silverman, Steven M.
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 without employing 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.