Synthesis study of 4-carbamoyl-4'-azide-1,2,3-triazole nucleoside derivatives
Objective This paper aimed to synthesize 4-carbamoyl-4'-azido-1,2,3-triazole to discover nucleoside drugs with high antiviral activity.Methods Using commercially available 1,2∶5,6-Di-O-isopropylidene-α-D-glucofuranose as the starting material,the important glycosyl azide compound was prepared through 9 steps.This intermediate was then subjected to a[3+2]dipolar cycloaddition reaction with methyl propiolate to construct a triazole ring.Finally,4-carbamoyl-4'-azide-1,2,3-triazole nucleoside was obtained by radical decarboxylative azidation reaction and deprotection.Results 4-Carbamoyl-4'-azide-1,2,3-triazole nucleoside was obtained through 5 steps in an overall yield of 30％,which laid a foundation for the later antiviral activity test.
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