Method for solid-phase synthesis of DS-8201 intermediate and preparation method of DS-8201

The invention relates to the technical field of medicine synthesis, in particular to a method for solid-phase synthesis of a DS-8201 intermediate and a preparation method of DS-8201. According to the method for solid-phase synthesis of the DS-8201 intermediate, the hydroxyl end of a compound 5 is coupled to solid-phase resin, then Fmoc-Phe-OH, a glycine analogue and 6-maleimide hexanoic acid or succinimide ester thereof are spliced in sequence, a linker fragment is rapidly and efficiently synthesized by using the solid-phase synthesis method, purification in each step is not needed in solid-phase synthesis, and the method is simple and convenient to operate and easy to implement. The linker with high purity can be obtained by only washing the residual reagent/raw material after the condensation in each step and finally cutting off the linker from the branch, and the method is simple in step, low in cost and suitable for industrial production. 本发明涉及药物合成技术领域，具体涉及一种固相合成DS-8201中间体的方法及DS-8201的制备方法。本发明的固相合成DS-8201中