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.
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Zihao Dai
Jianxing Liu
Naixing Wang
Organic Letters
University of Chinese Academy of Sciences
Shanghai Institute of Organic Chemistry
State Key Laboratory of Chemical Engineering
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Dai et al. (Fri,) studied this question.
www.synapsesocial.com/papers/69a528ecf1e85e5c73bf05aa — DOI: https://doi.org/10.1021/acs.orglett.6c00046