610785-40-5Relevant articles and documents
Preparation method of eplerenone with high efficiency and low pollution
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Paragraph 0037-0039; 0048-0050; 0059-0061, (2020/11/10)
The invention discloses a preparation method of eplerenone with high efficiency and low pollution, and belongs to the technical field of preparation and processing of steroid hormone drugs. The methodcomprises the steps: by taking a compound I, namely delta 9,11-canrenone, as an initial raw material, carrying out 7-furyl addition, furyl ring opening and lactonization cyclization reaction to obtain 5,7-lactone, and carrying out ring opening methylation and 9,11-double bond epoxidation reaction to obtain the eplerenone. According to the method, raw materials and reagents are cheap and easy to obtain, and the method has extremely high market competitiveness in equipment investment and production cost; reagents used in the method are low in environmental pollution, and particularly cyano-containing high-toxicity compounds are not used, so that the method is greener and more environment-friendly; the production process is easy to control, high in yield, low in cost and suitable for industrial production.
A new approach to the furan degradation problem involving ozonolysis of the trans-enedione and its use in a cost-effective synthesis of eplerenone
Pearlman, Bruce A.,Padilla, Amphlett G.,Hach, John T.,Havens, Jeffrey L.,Pillai, Muniraj D.
, p. 2111 - 2113 (2007/10/03)
Whereas ozonization of furan 3a affords little or no carboxylic acid 5, ozonization of the corresponding trans-enedione 6 afforded carboxylic acid 5 in 82.4% yield (cryst., overall from furan, 100 g scale; after workup with dimethyl sulfide, followed by mildly basic hydrogen peroxide). This new approach to furan degradation is showcased in a cost-effective synthesis of eplerenone, an important new medicine for cardiovascular indications.
Process to prepare eplerenone
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Page 46, (2008/06/13)
The present invention involves intermediates, including a 7α-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.