- 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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- 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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