Synthesis method of medroxyprogesterone acetate

The technology of a methadone and a synthetic method, which is applied in the field of pharmaceutical chemical synthesis, can solve the problems of high cost and low yield, and achieve the effects of reducing processing cost, good production safety, and easy recycling and reuse
CN102911233AInactive Publication Date: 2013-02-06BAOJI KANGLE BIOTECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
BAOJI KANGLE BIOTECH
Publication Date
2013-02-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthesis method of medroxyprogesterone acetate. The method comprises the following steps of: 1) enabling 17 alpha-hydroxyprogesterone and ethylene glycol to perform ketalation under the catalysis of para-toluenesulfonic acid to obtain a ketal; 2) enabling the ketal to perform epoxidation reaction under the action of a peroxyacetic acid solution of anhydrous sodium acetate to obtain an epoxide; 3) enabling the epoxide and methylmagnesium bromide to perform Grignard reaction, and then performing hydrolysis reaction by dilute sulphuric acid to obtain a Grignard matter; 4) performing hydrolysis on the Grignard matter by glacial acetic acid to perform deprotection so as to obtain 5 alpha, 17 alpha-dihydroxy-6 beta-methyl progesterone; 5) performing hydrogenation translocation reaction under the action of hydrogen chloride to obtain 6 alpha-methyl-17 alpha-hydroxyprogesterone; and 6) enabling the 6 alpha-methyl-17 alpha-hydroxyprogesterone to perform acetylation reaction with acetic acid and acetic anhydride so as to obtain the medroxyprogesterone acetate. During the reaction process of the method disclosed by the invention, the use of a precious metal catalyst, namely palladium on carbon is avoided, the cost of auxiliary materials and the recovery cost are greatly reduced, the reaction conditions in each step are mild, the violent heat release and deflation phenomena are avoided, and the safety in production is good.
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Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical chemical synthesis, and in particular relates to a method for synthesizing medroxyprogesterone. Background technique

[0002] Medroxyprogesterone, Chinese alias medroxyprogesterone acetate, medroxyprogesterone acetate, medroxyprogesterone ester, oxymedroxyprogesterone acetate, medroxyprogesterone, etc., is an important hormone drug, mainly used for dysmenorrhea , functional amenorrhea, functional uterine bleeding, threatened abortion or habitual abortion, endometriosis, treatment of advanced breast cancer, endometrial adenocarcinoma and kidney cancer, etc.

[0003] At this stage, most domestic companies adopt the classic synthetic route: 17α-hydroxyprogesterone acetate is used as raw material, etherified, McFarland reaction, hydrolyzed to generate 6-position methine, and then 6-position hydrogenation reaction to generate Medroxyprogesterone acetate.

[0004] Its synthetic route is as foll...

Claims

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