The invention relates to
fluorine-containing isoxazolidine-5-
ketone as well as a synthesis method and anti-tumor application thereof. According to the synthesis method, gem-difluorocycloacrylimide and
nitrone are taken as substrates, Ni (ClO4) 2.6 H2O is taken as a catalyst, (+ / -)-2, 2 '-(
propane-2, 2-diyl) bis (4-phenyl-4, 5-dihydrooxazole) is taken as a ligand (L) in an
organic solvent,
cycloaddition isomerization reaction is carried out at about 30 DEG C, and the
fluorine-containing isoxazolidine-5-
ketone compound is obtained. And the
fluorine-containing isoxazolidine-5-
ketone is obtained through preparation. The method is mild in reaction condition, capable of being well compatible with various functional groups and high in yield, and the product further has certain
biological activity and can inhibit proliferation of
cancer cells. The invention discloses the realization of the cycloisomerization reaction of the gem-difluorocyclopropene and the
nitrone for the first time, provides a new idea for the synthesis of the fluorine-containing isoxazolidine-5-ketone and the derivative thereof, and has a good application prospect in the fields of medicines and synthesis.