PROCESS FOR PREPARATION OF 1-ACYL-4-PHENYLSULFONYLPROLINAMIDE DERIVATIVES AND NEW INTERMEDIATES Russian patent published in 2017 - IPC C07D207/16 C07D401/12 C07D403/12 A61K31/401 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing proline of formula 1, where R¹ is selected from C_1-7-alkyl or a radical of formula II, where R⁴ is selected from a group, containing C_1-7-alkyl, halogen-C_1-7-alkyl and phenyl, optionally substituted by halogen; R² is selected from a group, containing halogen or halogen-C_1-7-alkyl; and R³ is selected from a group, containing hydrogen, halogen, halogen-C_1-7-alkyl, C_1-7-alkoxy, halogen-C_1-7-alkoxy or 5-or 6-member heterocycle, containing one or two nitrogen atoms, wherein cycle is optionally substituted with C_1-7-alkyl or halogen, and a novel intermediate compound used in method.

EFFECT: proline derivatives of formula 1 are preferable inhibitors of cysteic cathepsin protease S and are therefore useful in treating metabolic diseases, such as diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral artery disease and diabetic neuropathy.

29 cl, 1 ex