An Efficient Chemoenzymatic Process for Preparation of Ribavirin

Autor: Vladimir Sakharov, Sergey Baykov, Irina Konstantinova, Roman Esipov, Mikhail Dorogov
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Zdroj: International Journal of Chemical Engineering, Vol 2015 (2015)
Druh dokumentu: article
ISSN: 1687-806X
1687-8078
DOI: 10.1155/2015/734851
Popis: 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.
Databáze: Directory of Open Access Journals