FIELD: biotechnology.
SUBSTANCE: invention relates to the field of biotechnology. A group of inventions is described, including a one-pot method for preparing an intermediate product of an antibody-drug conjugate, where the intermediate product of an antibody-drug conjugate is Py-MAA-Val-Cit-PAB-D or MC-Val-Cit-PAB-D, the use of the above a method in the preparation of an antitumor drug; and the use of the above method in the preparation of an antibody-drug conjugate. In one embodiment, the method comprises reacting Py-MAA-Val-Cit-PAB-OH or MC-Val-Cit-PAB-OH with bis (4-nitrophenyl) carbonate (NPC) in the presence of an organic base with the further addition of organic base and adding 1-hydroxybenzotriazole and drug part D to the reaction system.
EFFECT: invention expands the arsenal of methods for obtaining intermediate products of the antibody-drug conjugate.
9 cl, 1 dwg, 1 tbl, 6 ex
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