IMPROVED MAITANZINOL ACYLATION METHODS Russian patent published in 2022 - IPC C07D498/18 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a method for obtaining a compound represented by the formula:

(Ia);

where R₁ is methyl; and R₂ is methyl; including the interaction of maitanzinol with N-carboxyanhydride in a reaction mixture additionally containing Lewis’ acid, a base and desiccant, while N-carboxyanhydride is represented by the following formula:

(IIa),

with the formation, thus, of a compound of the Formula (Ia), or including a) the interaction of maitanzinol with N-carboxyanhydride in a reaction mixture additionally containing Lewis’ acid and a base, while N-carboxyanhydride is represented by the following formula:

(IIa),

with the formation, thus, of a compound of the Formula (Ia), and b) the interaction of unreacted N-carboxyanhydride from the reaction mixture at the stage a) with a nucleophilic reagent, which is alcohol.

EFFECT: new methods are developed for the preparation of the compound Ia, which allow one to improve the yield and minimize the number of by-products formed during reactions used to produce it.

34 cl, 4 dwg, 1 tbl, 10 ex