The present invention provides a method for preparing a drug-linker MC-MMAF for use in an antibody-binding drug and an intermediate thereof. The present invention improved the reaction activity of the N-terminus, effectively controlling the occurrence of the racemization reaction. By not directly using the toxin MMAF, but by using a relatively low-toxic fragment peptide, the difficulty of mass production is reduced, and the operation is simple as there is no need for reverse-phase production.
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