The invention belongs to the pharmaceutical synthesis field, relating to iodinated linoleic acid deoxidation fluorouracil glucoside ester, a preparation method thereof and application of anticancer. In the invention, anticancer medicines are used as a warhead and the iodinated linoleic acid is used as a carrier to make a chemical covalent composition as a guiding therapy tumor medicine for recognizing cancer. The experiment shows that the medicine can be selectively adhered to and deposited in cancer tissues, and directly kill cancer cells partially for a long time with high concentration, and under the condition of slow degradation of internal esterase, the medicine can be released for 1-3 months to directly restrain cancer. The medicine and the traditional iodipin both belong to long-chain aliphatic ester, have similar physical and chemical characteristics, and can be mixed with other anticancer medicines to produce an emulsifier, for cancer embolism of blood vessel chemo-treatment, such as liver cancer, pancreatic cancer, rectal cancer, esophagus cancer, gastric cancer, breast cancer and lung cancer. The medicine can be used as the local therapeutic medicine for diseases such as carcinoid, giant hemangioma and the like.