METHOD FOR THE PREPARATION OF N-SUBSTITUTED BRIDGING 1,2,4-DIOXAZOLIDINES Russian patent published in 2023 - IPC C07D498/18 

FIELD: organic chemistry.

SUBSTANCE: method for obtaining N-substituted bridging 1,2,4-dioxazolidines of the general formula

where R¹=H, lower alkyl, C₆H₅CH₂, 4-FC₆H₄CH₂, 4-BrC₆H₄CH₂, 4-ClC₆H₄CH₂, CH₂CH=CH₂, (CH₂)₂C(O)OEt, R²=H, C(O)OEt, C(O)OCH₂CH=CH₂, C(O)OBu^t, C(O)CH₂C₆H₅, R³=H, 4-NO₂C₆H₄, R⁴=o-BrC₆H₅, CH₂CN, 1-adamantyl, 2-pyrazyl, n-CH₃C₆H₄, 2-furyl, 2-thiophenyl, NH₂, X=C(O), SO₂, which consists in the fact that 1,5-diketones of the general formula

where R¹, R² and R³ have the above meanings, are reacted with an aqueous solution of hydrogen peroxide and a hydrazide of the general formula NH₂NHXR⁴, where X and R⁴ have the above meanings, in methanol in the presence of an acid catalyst.

EFFECT: obtaining compounds containing in their structure a cyclic peroxide fragment and an N-substituted amino group, of general formula I in high yield, which can be used in medicine as antimalarial and anticancer agents.

3 cl, 36 ex