- Nomegestrol intermediate synthesizing method
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The invention provides a nomegestrol intermediate synthesizing method. The nomegestrol intermediate synthesizing method is characterized in that nomegestrol intermediate synthesis utilizes compound of 4-estrenochrysene-3,17-diketone as a beginning raw material; a nomegestrol intermediate crude product can be obtained through cyaniding, silyl etherification, intramolecular nucleophilic substitution reaction, reduction reaction and esterification reaction; then the nomegestrol intermediate can be obtained through methyl alcohol and ethyl acetate crystallization. The preparation method disclosed by the invention utilizes a short synthesizing line, the intermediate has stable performance, product yield is high, production cost is low, a production process is easy to control, environmental pollution is small, and industrial production is facilitated.
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- A PROCESS FOR THE PRODUCTION OF OF 19-NORPREGN-4-EN-3,20-DIONE-17.ALPHA.-OL (GESTONORONE) AND INTERMEDIATES THEREFOR
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The present invention relates to a new stereoselective process for the synthesis of 17(α)-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17(α)-17-acetyl-17-hy droxy-estr-4-en-3 -one (gestonorone) is an important intermediate in the synthesis of the active ingredients having progestogen activity - such as gestonorone capronate and nomegestroi acetate. Formulas (I), (II) and (III).
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- An improved synthesis of nomegestrol acetate
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Oral contraceptives (OCs) are synthetic steroids, or progestins, which are structurally related to testosterone or to progesterone. Many progestins have been synthesized and approved for OCs, hormonal replacement therapy (HRT), or the treatment of some gynecological disorders. Nomegestrol acetate (NOMAc) is a newly approved OC and has gained rapid acceptance in many countries for OC or HRT. The synthesis of NOMAc remains challenging and costly. We have developed a novel and improved procedure for the synthesis of NOMAc with a total of 11 steps and an overall good yield without the use of hazardous reagents.
- Lu, He-Lin,Wu, Zong-Wen,Song, Shu-Yong,Liao, Xiao-Dan,Zhu, Yan,Huang, Yun-Sheng
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p. 431 - 436
(2014/04/17)
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- Novel 17-esters of 17α-hydroxy gestogens, compositions containing such compounds, processes for their preparation and methods of treatment therewith
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This invention relates to novel 17α-esters of gestogens having an antitumour activity and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the said compounds, and method of treatment therewith.
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