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Efficient synthesis of nucleoside aryloxy phosphoramidate prodrugs utilizing benzyloxycarbonyl protection |
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| Authors: | Jong Hyun ChoFranck Amblard Steven J. CoatsRaymond F. Schinazi |
| Affiliation: | a Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine and Veterans Affairs Medical Center, Atlanta, GA 30033, USA b RFS Pharma, LLC, 1860 Montreal Road, Tucker, GA 30084, USA |
| Abstract: | An efficient method for the synthesis of nucleoside phosphoramidates prodrugs (6a-f) has been developed that employs a simple protection/deprotection sequence of the nucleoside with benzyloxycarbonyl (Cbz). The coupling reaction of Cbz-protected derivatives (5a-f) with phenyl-(ethoxy-l-alaninyl)-phosphorochloridate (7), followed by Cbz group removal by hydrogenolysis provided the phenyl phosphoramidate ProTides (6a-f) in excellent overall yields. |
| Keywords: | ProTide Nucleoside Monophosphate prodrug Benzyloxycarbonyl Antiviral |
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