METHOD OF PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1,6-NAPHYRIDINE-3-CARBOXAMIDE BY SEPARATION OF THE RACEMATE USING A DIASTEREOMERIC COMPOSITE TARTARIC ACID ESTER Russian patent published in 2023 - IPC C07D471/04 

Abstract RU 2805573 C2

FIELD: medicine.

SUBSTANCE: invention relates to a method of separating racemate (II) into (Ia) and/or (I) using chiral substituted tartaric acid esters of general formulas (IIIa) or (IIIb), where Ar is

where * denotes the connection point, at the temperatures ranging from 60 to 80°C, with the formation of diastereomeric salts (IVa), (IVb), (IVc) and/or (IVd), which is carried out in mixtures of solvents consisting of water and miscible organic solvents with water.

EFFECT: technical result is a new method of separating racemate (II) which can be used to obtain (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of formula (I) with high yield and purity, which has the effect of a non-steroidal mineralocorticoid receptor antagonist and can be used in medicine as a means for the prevention and/or treatment of cardiovascular and renal diseases.

16 cl, 1 dwg, 8 tbl, 9 ex

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RU 2 805 573 C2

Authors

Platzek, Johannes

Lovis, Kai

Joentgen, Winfried

Dates

2023-10-19Published

2019-04-23Filed