FIELD: chemistry.
SUBSTANCE: invention relates to a method for producing an antibody-drug conjugate of formula (I), wherein Ab is an antibody or an antigen-binding fragment thereof; D is eribulin; m is integer of 1–10; and p is integer 1–8, wherein said method comprises: (i) reacting a compound of formula (1), where m in Formula (1) is integer from 1 to 10, with a compound of Formula (2) to obtain a compound of Formula (3), (ii) acylation of the hydroxyl group in the compound of Formula (3) using an acylating agent, and where the acylating agent includes a phenoxy group or a nitrophenoxy group, thereby obtaining a compound represented by Formula (A), (iii) reacting eribulin or a salt thereof with a compound represented by Formula (A) to obtain a compound, represented by Formula (B), (iv) reacting a compound represented by Formula (B) with an antibody or an antigen-binding fragment thereof to obtain an antibody-drug conjugate represented by Formula (I).
EFFECT: method provides preparing the high-yield antibody-drug conjugate.
10 cl, 10 tbl, 4 ex
Formula (I)
Formula (1)
Formula (2)
Formula (3):
Formula (A)
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