Journal
ORGANIC LETTERS
Volume 19, Issue 9, Pages 2218-2221Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b00469
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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.
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