Synthesis of acyclovir as an antiherpes-virus drug

Tran Quang Hung, Nguyen Thi Thuong, Tran Van Sung
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Authors

  • Tran Quang Hung
  • Nguyen Thi Thuong
  • Tran Van Sung

DOI:

https://doi.org/10.15625/4633

Abstract

A one-pot process for high-yield regioselective synthesis of 9-[(2-hydroxyethoxy) methyl]guanine (acyclovir),  an antiherpetic agent, was achieved from guanine via the steps of reacting of N2,N9 -diprotected guanine with 1-acetyl-2-acetylmethoxy-ethyleneglycol in presence of phosphoric acid or polyphosphoric acid. Total yield of product was 59%. The obtained acyclovir meets the standards in the British Pharmacopoeia 2007 (BP2007). Its activity as inhibitor of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) was evaluated according to the plaque reduction assay method and compared with the standard compound. The synthesized acyclovir showed a similar activity as the control.

Keywords: Acyclovir, Herpes simplex virus, Nucleoside, One- pot synthesis.

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Published

27-08-2014

How to Cite

Hung, T. Q., Thuong, N. T., & Sung, T. V. (2014). Synthesis of acyclovir as an antiherpes-virus drug. Vietnam Journal of Chemistry, 47(4), 523. https://doi.org/10.15625/4633

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