95716-70-4Relevant articles and documents
Preparation method of eplerenone intermediate delta 9, 11 alkenyl ester
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Paragraph 0050; 0054; 0055; 0064-0073; 0076; 0077, (2020/02/10)
The invention provides a preparation method of eplerenone intermediate delta 9, 11 alkenyl ester, and the method comprises the following steps: carrying out esterification reaction on raw materials and methanesulfonyl chloride to generate methanesulfonate; and carrying out elimination reaction on the methanesulfonate to obtain an eplerenone intermediate; the method has the advantages that the process yield is about 90%, and the product purity is obviously higher than that reported in the existing literature. The delta 11, 12-alkenyl ester generated in the method has the advantages of fewer lactone impurities and high yield, and the method is an economic and environment-friendly synthetic route, greatly improves the prior art, and is suitable for industrial production.
Method for synthesizing 7a-methyl formate-9(11)-encanrenone
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, (2020/05/01)
The invention discloses a method for synthesizing 7a-methyl formate-9(11)-encanrenone. The method comprises the following steps: reacting 9(11)-encanrenone used as a raw material with 2-methylfuran atfirst, performing ring opening by using dibromohydantoin, rearranging, ozonizing, adding a metal reducing agent to methanol or a mixed solution of methanol and other solvent, and performing reducingesterification to directly obtain the 7a-methyl formate-9(11)-encanrenone. The method has the advantages of operation step simplification, high yield, simplicity in operation, few three wastes, and suitableness for industrial production.
PROCESS FOR THE PREPARATION OF 7 alpha -(METHOXYCARBONYL)-3-OXO-17alpha-PREGN-4,9(11)-DIEN-21,17-CARBOLACTONE, A USEFUL INTERMEDIATE FOR THE SYNTHESIS OF MOLECULES WITH PHARMACOLOGICAL ACTIVITY
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Paragraph 0040; 0041; 0042; 0043; 0044, (2016/05/10)
An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.