A method for preparing a racemate of finerenone

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A method for preparing a racemate of finerenone
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                        CAO Yang1CAO Yang
School of Chemistry and Chemical Engineering, Nanjing University
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CUI Wen-hui2CUI Wen-hui
Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Jiangsu Ocean University
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LI Qian2LI Qian
Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Jiangsu Ocean University
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WU Qing-kun2WU Qing-kun
Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Jiangsu Ocean University
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GAO, Hui2GAO, Hui
Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Jiangsu Ocean University
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Affiliation:1.School of Chemistry and Chemical Engineering, Nanjing University;2.Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Jiangsu Ocean University
Clc Number:O621.3
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Abstract:

Using 4-cyano-3-methoxybenzaldehyde and tert-butyl acetoacetate as raw materials, finerenone racemes were obtained through condensation, cyclization, oxyalkylation, hydrolysis and ammonolysis, which broke through the difficulty of hydrolysis of conventional esters. A series of optimization of reaction conditions were carried out, and the finerenone racemes were obtained with a total yield of 33.5%. The results showed that the reaction conditions were mild and the yield was high, which provided a reasonable route for the synthesis of finerenone raw materials. The structure of the product was determined by 1 HNMR, 13CNMR and HRMS.

Key words:Finerenone; Optimization of route; Diabetic Nephropathy; Active Pharmaceutical Ingredient

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Received:October 12,2023
Revised:December 23,2023
Adopted:December 11,2023
Online: November 08,2024
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