The invention provides a benzoxazinorifamycin derivative. The chemical structural formula of the benzoxazinorifamycin derivative is as shown in the description. The benzoxazinorifamycin derivative hasexcellent antibacterial properties, has excellent antibacterial effects on common bacterial strains, simultaneously has good antibacterial effects on some drug-resistance bacteria, makes up for lackof existing related drugs, and can provide a certain basis for the next step in researches and developments of antibacterial drugs. The invention also provides a benzoxazinorifamycin derivative preparation method and use of the benzoxazinorifamycin derivative in the aspect of preparation of antibiotic drugs.