| abstract |
Provided is a method for producing an antibody-drug conjugate intermediate by addition of acid. An acid additive is used to convert the monomethyl auristatin derivative into a salt thereof to participate in the reaction. The addition of the acid additive can significantly improve the yield of the final product. In addition, the low price of the acid additive greatly reduces the production cost of the final ADC product. Moreover, the method of the present invention adopts a one-step preparation process, in addition to a higher yield of the final product, not only reducing the cost of the consumables, labor, equipment, site, raw materials and the like in the production, but also greatly reducing the production of the waste liquid, and thus reducing production costs and improving production efficiency, and making the method suitable for industrial large-scale production. |