合成路线1

This compound has been obtained by several related ways: The acylation of Ribavirin (1-(beta-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide) (I) with Ac2O gives the triacetate (II), which is anhydrized by means of POCl3 and TEA in chloroform to yield the carbonitrile (III). The reaction of (III) with NaOMe in methanol affords the methyl carboximidate (IV), which is finally treated with NH4Cl and NH3 in methanol to provide the target carboxamidine. Alternatively, the intermediate carbonitrile (III) can be treated with NH4Cl and NH3 in methanol at 85 C in a steel bomb to give the target carboxamidine. Finally, the condensation of 1,2,3,5-tetra-O-acetyl-beta-D-ribofuranose (V) with 1,2,4-triazole-3-carbonitrile (VI) by means of bis-(4-nitrophenyl)phosphate (BNPP) at 150 C also gives the intermediate triacetyl carbonitrile derivative (III).