The application discloses 4,8-
epoxy-1,3-
dioxolane[4,5-d]-1,2-
diazole compounds and a preparation method and application thereof, belongs to the technical field of medicines, and particularly relates to 4,8-
epoxy-1,3-
dioxolane[4,5-d]-1,2-
diazole compounds, a preparation method thereof, and application thereof in preparation of antitumor drugs. The structural general formula of the 4,8-
epoxy-1,3-
dioxolane[4,5-d]-1,2-
diazole compounds is as follows: wherein R1 is selected from C1-C4
alkyl, C3-C6 cycloalkyl, benzyl, methoxy-substituted benzyl,
halogen-substituted benzyl, phenyl, C1-C4
alkyl-substituted phenyl, hydroxyl-substituted
alkyl, and ethoxycarbonylmethyl; and R2 is selected from
hydrogen, C1-C4 alkyl, and benzyl. The 4,8-epoxy-1,3-dioxolane[4,5-d]-1,2-diazole compounds provided by the method have novel structures, many modifiable sites, mild
reaction conditions, cheap and readily available raw materials, few steps, simple operation, good
stereoselectivity, a simple synthesis method, and are suitable for industrialized production.