MESYLATE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONOHYDRATE Russian patent published in 2017 - IPC C07D417/12 

FIELD: chemistry.

SUBSTANCE: invention relates to a method for production of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide, and as its mesylate monohydrate salt, which showed improved stability and release kinetics of pharmaceutical compositions. The method is implemented in accordance with steps A and B. On step A, interation of the common formula A* compound takes place, where R¹ represents a leaving group and R² represents an alkyl residue containing 1 to 6 carbon atoms or a cycloalkyl residue containing 3 to 6 carbon atoms, with a boronic acid derivative, borolan, borinan or diboronic acid reagent toprovide an intermediate boronic acid derivative of compound A, and then the intermediate boronic acid derivative reacts with a pyridine B compound of the common formula B*, where R³ represents a leaving group, under basic conditions for direct preparation of (4-pyridin-2-yl-phenyl)acetic acid, which is then purified. Step B includes interaction of (4-pyridin-2-yl-phenyl)acetic acid obtained on Step A with 4-methyl-2-(methylamino)-1,3-thiazole-5-sulfonamide to obtain N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide. .

EFFECT: method allows simplified target compound synthesis, reduced number of steps, as well as increased yield.

8 cl, 3 dwg, 5 tbl, 8 ex