Method for synthesizing steroid progestogen

A progesterone and steroid technology, applied in the field of medicinal chemistry, can solve the problems of low yield and achieve high yield, low cost, and large-scale industrial production value
CN1865276AInactive Publication Date: 2006-11-22JIANGSU CHUANGUO PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JIANGSU CHUANGUO PHARMA CO LTD
Publication Date
2006-11-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthetic method of steroidal gestagen and key medium I, II, III, IV in the drug chemical technological domain, which adopts 13 ethyl- 1,3,5(10),8(9)- estrange tetraenes-17-alcohol as raw material to synthesize deoxidation pregnancy and depending pregnancy.
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Description

Technical field:

[0001] The invention belongs to the technical field of medicinal chemistry. In particular it relates to methods for the synthesis of steroidal progestogens. Background technique:

[0002] 13β-Ethyl-11-Methylene-18.19-Dianox-17α-Pregn-4-ene-20-Ethynyl-17β-Hydroxy is a steroidal progestin contraceptive that can inhibit ovulation and gonadotropin Secretion, the trade name is Marvelon. 13β-ethyl-11-methylene-18.19-bisanox-17α-pregnant-4-en-3-ketone-20-ethynyl-17β-hydroxyl is a derivative of desogestrel, and the Netherlands Organon company will It was developed into a single-root subcutaneous sustained-release long-acting contraceptive implant with the trade name Implanon. Its synthetic route has following several kinds:

[0003] (1) Synthesis of 13β-ethyl-11-methylene-18.19-bisanth-17α-pregna-4-ene- from 11-hydroxyestr-5-ene-3,17-dione 20-ethynyl-17β-hydroxyl, see reaction formula 1:

[0004]

[0005]

[0006] Reaction one ...

Claims

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