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International Journal of Chemical Engineering
Volume 2015, Article ID 734851, 5 pages
Research Article

An Efficient Chemoenzymatic Process for Preparation of Ribavirin

1Ushinsky Yaroslavl State Pedagogical University, Yaroslavl 150000, Russia
2Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow 117997, Russia

Received 30 July 2015; Revised 11 October 2015; Accepted 26 October 2015

Academic Editor: M. G. Ierapetritou

Copyright © 2015 Vladimir Sakharov et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Ribavirin is an important antiviral drug, which is used for treatment of many diseases. The pilot-scale chemoenzymatic process for synthesis of the active pharmaceutical ingredient Ribavirin was developed with 32% overall yield and more than 99.5% purity. The described method includes the chemical synthesis of 1,2,4-triazole-3-carboxamide, which is a key intermediate and enzyme-catalyzed transglycosylation reaction for preparation of the desired product. 1,2,4-Triazole-3-carboxamide was synthesized from 5-amino-1,2,4-triazole-3-carboxylic acid by classical Chipen-Grinshtein method. Isolated from E. сoli BL21(DE3)/pERPUPHHO1 strain the purine nucleoside phosphorylase was used as a biocatalytical system. All steps of this process were optimized and scaled.