Design, synthesis, and characterization of new 5-fluorocytosine salts

Sathyanarayana R. Perumalla, Venkateswara R. Pedireddi, Changquan C. Sun

Research output: Contribution to journalArticle

24 Scopus citations

Abstract

5-Fluorocytosine (FC), an antifungal drug and a cytosine derivative, has a complex solid-state landscape that challenges its development into a drug product. A total of eight new FC salts, both cytosinium and hemicytosinium, with four strong acids were prepared by controlling acid concentration in the crystallization medium. The pharmaceutically acceptable saccharin salt of FC exhibits superior phase stability and, hence, has the potential to address the instability problem of FC associated with hydration.

Original languageEnglish (US)
Pages (from-to)2462-2466
Number of pages5
JournalMolecular pharmaceutics
Volume10
Issue number6
DOIs
StatePublished - Jun 3 2013

Keywords

  • 5-fluorocytosine
  • cytosine protonation
  • fluocytosine
  • hemicytosinium duplexes
  • nucleobase

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