Title: Telbivudine
CAS Registry Number: 3424-98-4
CAS Name: 1-(2-Deoxy-b-L-erythro-pentofuranosyl)-5-methyl-2,4(1H,3H)-pyrimidinedione
Additional Names: 1,2¢-deoxy-b-L-ribofuranosylthymine; 2¢-deoxy-L-thymidine; LdT; L-thymidine
Molecular Formula: C10H14N2O5
Molecular Weight: 242.23
Percent Composition: C 49.58%, H 5.83%, N 11.56%, O 33.03%
Literature References: Nucleoside analog; specific inhibitor of hepatitis B virus (HBV) replication. Prepn: J. Smejkal, F. Sorm, Collect. Czech. Chem. Commun. 29, 2809 (1964); A. Holy, ibid. 37, 4072 (1972). Anti-HBV activity: M. L. Bryant et al., Nucleosides Nucleotides Nucleic Acids 20, 597 (2001). In vitro pharmacology: B. Hernandez-Santiago et al., Antimicrob. Agents Chemother. 46, 1728 (2002). Clinical evaluation in hepatitis B: C.-L. Lai et al., Hepatology 40, 719 (2004). Review of mechanism of action and pharmacology: D. N. Standring et al., Antiviral Chem. Chemother. 12, Suppl. 1, 119-129 (2001); of clinical development: S.-H. B. Han, Expert Opin. Invest. Drugs 14, 511-519 (2005). See also Thymidine.
Properties: Crystals from ethanol, mp 186°(Smejkal, Sorm). [a]D20 -20.3° (c = 0.192 in water). Also reported as mp 189° (Holy). uv max (pH 2): 267 nm (e 9800).
Melting point: mp 186°; mp 189°
Optical Rotation: [a]D20 -20.3° (c = 0.192 in water)
Absorption maximum: uv max (pH 2): 267 nm
Therap-Cat: Antiviral.
Keywords: Antiviral; Purines/Pyrimidinones. |