METHOD FOR PRODUCING AN INHIBITOR OF THE COAGULATION FACTOR XIA AND AN INTERMEDIATE THEREOF Russian patent published in 2022 - IPC C07C235/38 C07C309/66 C07D213/69 A61K31/4418 

FIELD: chemistry.

SUBSTANCE: invention relates to a method for producing an inhibitor of the coagulation factor XIa and an intermediate thereof, in particular, to a method for producing a compound by the formula AI. The method includes a stage of conducting a reaction of a compound by the formula III with a compound by the formula II:

wherein ring A constitutes a 6-membered aryl; all R₁ are different and selected from a halogen and -C(O)R₅; R₂ constitutes a C₁-C₆alkoxy; L₁ constitutes an alkylene, wherein said alkylene may be additionally substituted with one or more substituents selected from a deuterium atom; all R₃ are the same or different, and each is independently selected from -C(O)OR₆; R₄ is selected from the group consisting of a C₁-C₆alkoxy and a 6-membered aryl; R₅ constitutes a C₁-C₆alkyl; R₆ constitutes a carboxy protecting group; LG constitutes a leaving group, such as substituted sulphonyloxy; n equals 2; s equals 1. Also proposed are intermediate compounds.

EFFECT: advantages of the proposed method include a high yield, good purity of the products, and mild reaction conditions.

24 cl, 4 ex