FIELD: cytotoxic benzodiazepine derivatives.
SUBSTANCE: invention is related to a method for producing a compound of formula (IIIA) or a salt thereof. The method includes steps (a) and (b). In step (a), a compound of formula (Ia) or a salt thereof is reacted with a compound of formula (a) or a salt thereof (eg an HCl salt) to form a compound of formula (IIa). In step (b), a compound of formula (IIa) is reacted with a carboxylic acid deprotectant to form a compound of formula (IIIa) wherein E is -OH, a halide or C(=O)E is an activated ester; P1 represents a carboxylic acid protecting group. The proposed method improves the production of indolinobenzodiazepine dimers and is more efficient and suitable for large-scale production.
EFFECT: invention is also related to a method for producing a compound of formula (Va) using the specified method.
32 cl, 5 ex
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