(2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID Russian patent published in 2020 - IPC C07D263/34 A61K31/421 A61P9/12 

FIELD: chemistry; medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound having structure (I), or a pharmaceutically acceptable salt thereof. Compound (I) is obtained by combining ethyl ether of (2R,4R)-4-amino-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxypentanoic acid with 5-methyloxazole-2-carboxylic acid. In crystalline form compound (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid is obtained by (a) combining ethyl ether of (2R,4R)-4-amino-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxypentanoic acid with 5-methyloxazole-2-carboxylate sodium to obtain (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid; (b) treating (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid with ethyl acetate and hexane until complete dissolution; and (c) recovering the obtained solid substance at room temperature.

(I)

EFFECT: compound (I) has activity which inhibits neprilysin and aims at treating hypertension, pulmonary hypertension, cardiac failure or renal insufficiency.

31 cl, 5 dwg, 1 tbl, 4 ex