METHODS FOR PRODUCING INDOLINOBENZODIAZEPINE DERIVATIVES Russian patent published in 2022 - IPC C07D487/04 

FIELD: chemistry.

SUBSTANCE: invention relates to methods for producing indolinobenzodiazepine monomer precursors, namely to a method for producing a compound of the formula (I) or its salt, including bringing into interaction a compound of the formula (II) or its salt with Fe in the presence of NH₄Cl, where R₁, R₂, R₃ and R₄, each independently, is -H; R₅ is OR, where R is selected from (C₁-C₃)alkyl. The invention also relates to a method for producing a compound of the formula (III) or its salt, including bringing into interaction the compound of the formula (I) or its salt with a hydrogenating agent in the presence of a palladium catalyst, where the hydrogenating agent is 1,4-cyclohexadiene; the palladium catalyst is Pd/Alox catalyst; R₁, R₂, R₃ and R₄, each independently, is -H; R₅ is -OR, where R is selected from (C₁-C₃)alkyl.

EFFECT: methods for producing indolinobenzodiazepine monomer precursors are developed that are more effective and suitable for large-scale process of production of cytotoxic indolinobenzodiazeoine dimeric compounds.

85 cl, 3 ex