Paper
CHEN Ziqi, HUANG Lei, FU Cuiping, LUO Kun, WANG Guan,
In this study, a novel synthetic process of finerenone(1), an anti-diabetic nephropathy drug, was
developed. Using 2-hydroxyethyl methyl sulfone(20) and 2,2,6-trimethyl-4H-1,3-dioxin-4-one(21) as starting materials,
the target product 1 was synthesized through sequential steps including alcoholysis, Knoevenagel condensation, Hantzsch
cyclization, etherification, chiral resolution, β-elimination, and ammonolysis, with an overall yield of 19.9% (based on 20),
purity of 99.80% , and ee value of 99.82% . The novel process features mild reaction conditions and well-controlled quality,
yielding intermediate 2-(methylsulfonyl)ethyl (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-
1,6-naphthyridine-3-carboxylate with high optical purity following resolution, making it suitable for industrial production.