Finerenone

China [CN]

Synthesis and Quality Control Highlights

1. Synthesis Route (Core Steps)

Starting with 4-cyano-2-methoxybenzaldehyde as the raw material, S-configuration finerenone is obtained through condensation, chiral reduction, cyclization, and amidation; key steps: chiral reduction (controlling the proportion of S-configuration), and naphthyridine ring cyclization (improving yield).

2. Key Quality Control Items

Quality Control Item | Standard Requirements

Chemical Purity | HPLC purity > 99.5%

Impurity Control | Single impurity < 0.1%, total impurities < 0.5% (Key points: chiral isomers, oxidation byproducts)

Residual Solvents | Methanol < 3000 ppm, Dichloromethane < 600 ppm, Ethyl acetate < 5000 ppm

Moisture Content | Karl Fischer method < 0.5%

Chiral Purity | S-configuration > 99.5%, R-configuration impurity < 0.1%

Dissolution | ≥ 85% dissolution in 120 minutes (pH 6.8 medium)