The application belongs to the technical field of organic compound preparation, and discloses a tryptanthrin compound and a preparation method and application thereof. The preparation method of the tryptanthrin compound is that an indole-2,3-dione derivative, 2H-thieno[3,2-D][1,3]oxazin-2,4(1H)-dione, triethylamine and toluene are reacted to obtain the tryptanthrin compound. The tryptanthrin compound obtained by the method has a novel structure, shows an anti-ulcerative colitis activity, and has a potential to be developed into an anti-ulcerative colitisdrug.