- Novel intramolecular aminohydroxylation toward the syntheses of 2′-amino-2′-ethynyl nucleosides
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Syntheses of both 2′-amino-2′-ethynyl guanosine and uridine, using an intramolecular aminohydroxylation reaction as the key step, are described. The corresponding 5′-O-triphosphates of the aforementioned nucleosides were obtained and the inhibitory activity was subsequently evaluated against the hepatitis C virus NS5B polymerase.
- Huang, Yuhua,Bennett, Frank,Buevich, Alexei,Girijavallabhan, Vinay,Kerekes, Angela D.,Huang, Hsueh-Cheng,Tawa, Paul,Bogen, Stephane L.,Davies, Ian W.
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- 2 -ALKYNYL SUBSTITUTED NUCLEOSIDE DERIVATIVES FOR TREATING VIRAL DISEASES
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The present invention relates to 2'-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2'-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
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(2014/06/11)
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