Synthesis of ( S )-Finerenone via Late-Stage Asymmetric Transfer Hydrogenation

Herein, we report a convergent and practical synthesis of the nonsteroidal mineralocorticoid receptor antagonist (S)-finerenone. The present approach incorporates a scalable, chromatography-free method to attain a racemic precursor with an impressive overall yield of 88%. Leveraging this versatile intermediate, we have developed two complementary approaches, including a robust resolution utilizing (+)-benzoyl tartaric acid and an efficient asymmetric transfer hydrogenation facilitated by chiral phosphoric acid-catalyzed dynamic kinetic resolution (DKR), to avoid cumbersome purification procedures, thereby offering a flexible, high-yielding, and highly enantioselective platform for the industrial-scale production of (S)-finerenone.