- Method for synthesizing flurogestone acetate
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The invention relates to the field of medicament synthesis, and discloses a method for synthesizing flurogestone acetate. The method is characterized by comprising the following steps: (1) synthesis of FPA-3; (2) synthesis of FPA-4; (3) synthesis of FPA-5; (4) synthesis of FPA-6. The method has the advantages of short synthesis route, low synthesis cost and high process controllability, and higher yield and purity of a prepared product.
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Paragraph 0068; 0114-0125
(2017/10/13)
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- Preparation method of flurogestone acetate
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The invention discloses a preparation method of flurogestone acetate. The preparation method comprises the following steps: using 9a-cortisone bifluoride as a raw material, dissolving 9a-cortisone bifluoride into an organic solvent, and reacting with acyl chloride under the existence of an acid-binding agent to obtain a 9a-cortisone bifluoride-21-O-ester; then reacting the ester with sodium iodide and a sulfur-containing reducing agent in the organic solvent for deesterification, and synthesizing flugestone; and finally reacting the flugestone with acetylchloride or acetic anhydride in the organic solvent, and synthesizing flurogestone acetate. According to the preparation method, 9a-cortisone bifluoride is used as the raw material, flurogestone acetate is synthesized through three-step reaction of 21-site esterification, then reduction and de-esterification and finally 17-site ethyl esterification, and compared with a traditional synthetic method for using a mold removal object acquired through diosgenin processing as a raw material, the preparation method has the advantages such as wide raw material source, short synthetic route, simple, convenient and environmentally-friendly process, few invested equipment and high product yield, and the production cost in the method is reduced by 25% to 30% as compared with a traditional method; and a solvent used in the production can be recycled and circularly used, and is easy for industrial production.
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Paragraph 0013; 0014; 0015
(2017/12/13)
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