Preparation method of antibody coupling drug toxin Duostatin-5

The invention discloses a preparation method of an antibody-coupled drug toxin Duostatin-5. The synthesis route of the antibody-coupled drug toxin Duostatin-5 is as shown in the following formula. The specific preparation method comprises the following steps: performing dehydration condensation on a compound A and DMT to obtain an intermediate B, performing deprotection on a protecting group ester group of the compound B to obtain an intermediate C, performing condensation on the intermediate C and a compound 2 to obtain an intermediate 5, and performing deprotection on the intermediate 5 to obtain Duostatin-5. The novel preparation method is simple in process, good in safety performance, high in product yield and purity and easy to realize large-scale production. 本发明公开了一种抗体偶联药物毒素Duostatin-5的制备方法，其合成路线如下所式。具体的制备方法包括:将化合物A和DMT脱水缩合得中间体B，将化合物B的保护基酯基脱保护得中间体C，中间体C与化合物2缩合得中间体5，中间体5再脱除保护得Duostatin-5。新的制备方法工艺简单，安全性能好，产品收率和纯度高且容易实现规模化生产。