Preparation method of norethindrone acetate

A technology of norethisterone acetate and a synthesis method is applied in the field of drug preparation, can solve the problems of large 3-position acetylenic impurities, is unsuitable for industrial production, difficult to purify and the like, achieves mild reaction, is suitable for industrial production and operation low cost effect
CN111875656AInactive Publication Date: 2020-11-03ZHEJIANG SHENZHOU PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHEJIANG SHENZHOU PHARMA
Publication Date
2020-11-03
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of norethindrone acetate, and belongs to the technical field of preparation and processing of medicines. According to the method, 19-nor-4-rostenedione isused as an initial raw material, and the norethindrone acetate is prepared through four steps of protection, ethynylation, hydrolysis and esterification. According to the preparation method of norethindrone acetate, the defects of a traditional process are overcome, reaction conditions are mild, and formation of impurities is reduced; the method is high in overall conversion rate, simple and convenient to operate, suitable for industrial production and wide in market prospect.
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Description

technical field

[0001] The invention relates to the technical field of preparation of medicines, in particular to a preparation method of norethindrone acetate. Background technique

[0002] Norethindrone acetate, the English name is Norethisterone Acetate, the chemical name is 17α-ethynyl-17β-hydroxyestr-4-en-3-one 17-acetate, it is a derivative of 19-desmethyltestosterone, and it is a An orally effective progesterone that can inhibit the secretion of luteinizing releasing hormone in the hypothalamus and act on the pituitary gland to reduce its sensitivity to luteinizing releasing hormone, thereby blocking the release of gonadotropin and producing ovulation inhibition, therefore It is mainly used in combination with ethinyl estradiol as a short-acting oral contraceptive.

[0003] The synthesis method of norethindrone included in the "National Compilation of Raw Materials Processes" uses 19-nor-4-androstenedione as a starting material to obtain norethindrone by direct acety...

Claims

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