A series of new 3-(4-β-D-allopyranosyloxyphenyl)-4-[(un)substituted anilinocarbonyl]-5-meth- oxycarbonyl-isoxazoline derivatives have been synthesized by the condensation between 4-β-D-allopyranosy- loxy-α-chloro-benzaldehydeoxime and N-[(un)substituted phenyl]maleimides with triethylamine in the metha-nol through a 1,3-dipolar cycloaddition reaction. The structures of all the new compounds were established by 1H NMR, IR, and MS (HRMS) techniques. The preliminary bioassay test of 4a～4h and 5a suggested that some of these compounds should show good calm activity. For example, compounds 4b (200 mg•kg－1), 4c (200 mg•kg－1) and 4h (200 mg•kg－1) were better than the parent helicid.

Key words: 1,3-dipolar cycloaddition, isoxazoline, synthes, helicid