The invention relates to the technical field of
medicine synthesis, and particularly discloses a synthesis method of besudil
mesylate. The besudil
mesylate is prepared by taking 3-(4-chloroquinazoline-2-yl)
phenyl acetate and 5-amino-1H-
indazole-1-tert-
butyl formate as initial raw materials through four-step reaction, compared with the traditional process, the reaction
route is obviously simplified, the yield loss caused by accumulation of multi-step reaction can be effectively reduced, and the yield of besudil
mesylate is increased. And the complexity and the operation difficulty of the synthesis process are reduced. Meanwhile, the intermediate compounds B, C and D all have Boc protecting groups, so that the reaction in each step has higher selectivity, and the purity of the target product is favorably improved. In addition, the synthetic
route provided by the invention is mild in reaction condition, the safety of the process can be effectively improved, the
reaction energy consumption is reduced, the adopted
reagent is relatively environment-friendly, the treatment is relatively easy after the reaction is finished, serious
pollution to the environment is avoided, and the industrial prospect is high.