The study demonstrates Evans’ (R)-4-benzyl-2-oxazolidinone auxiliary enables efficient asymmetric synthesis of finerenone, achieving stereoselective naphthyridine core construction with 86:14 dr and 80% yield. Subsequent ammonia-mediated transamidation of the ethyl ester completes finerenone formation.

This article reports a new application of Evans’ chiral auxiliary for an efficient asymmetric synthesis of finerenone. This new application successfully achieves the key step of stereoselective construction of the naphthyridine core of finerenone, with a high diastereomeric ratio (dr 86:14) and an 80% yield of the desired product via Evans’ chiral (R)-4-benzyl-2-oxazolidinone. The downstream transamidation of ethyl ester, with ammonia, leads to the formation of finerenone.