SYNTHESIS OF ARYL COMPOUNDS Russian patent published in 2021 - IPC C07C2/64 A61P31/04 C07C15/46 C07C15/52 C07C2/68 C07C2/70 C07C5/09 

FIELD: pharmaceutics.

SUBSTANCE: method is proposed for the synthesis of a compound of the Formula (1) or its pharmacologically acceptable salt of the Formula (1), where n is 2-6, and each R₁ is independently selected from -NR^aR^b, where R^a is H, and R^b is H or C_1-4 alkyl; or $$$ , where n is 1-8, and R^a is H, and R^b is selected from H or C_1-4 alkyl; or -C(O)OR^a or -(CH₂)_mC(O)OR^a, where m is 1, 2, 3, 4, 5, 6, 7 or 8, each R^b is independently selected from H or C_1-4 alkyl and each R^a is independently selected from H or C_1-4 alkyl; where the method includes following steps: (i) the introduction of a compound of the Formula (2) into the reaction, where n is 2-6, and X is halogen; with a compound of the Formula (3), where Y is -B^K-G₃M⁺; G is halogen; M is any metal of a group (I); and K is 1 or 2; under reaction conditions from the first set in the presence of palladium catalyst and a base to obtain a compound of the Formula (4), where n is 2-6; and (ii) the introduction of a compound of the Formula (4) into the reaction with one, two, three or four compounds of the formula (5), where D is halogen, metal halide of the Group I or Group II, triphthalate or -N₂⁺BF₄^-, and R₁ is independently selected from -NR^aR^b, where R^a is H, and R^b is H or C_1-4 alkyl; or $$$ , where n is 1-8, and R^a is H, and R^b is selected from H or C_1-4 alkyl; or -C(O)OR^a or -(CH₂)_mC(O)OR^a, where m is equal to 1, 2, 3, 4, 5, 6, 7 or 8, each R^b is independently selected from H or C_1-4 alkyl and each R^a is independently selected from H or C_1-4 alkyl; under the conditions of the reaction from the second set in the presence of palladium catalyst and a base to obtain a compound of the Formula (1).

EFFECT: technical result is the development of an effective and large-scale synthesis of a therapeutic drug.

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21 cl, 7 ex