13β-Ethyl-17α-Hydroxy-11-Methylene-,Cyclic 1,2-Ethanediyldithioacetal-18,19-Dinorpregn-4-En-20-Yn-3-One置于水体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 2.5H,以98%的收率获得产物依托孕烯 参考文献: Combined Synthesis Route For Etonogestrel And Desogestrel[fr] Voie De Synthèse Combinée De L'étonogestrel Et Du Désogestrel 标题: Combined Synthesis Route For Etonogestrel And Desogestrel[fr] Voie De Synthèse Combinée De L'étonogestrel Et Du Désogestrel 摘要:本发明涉及一种合成路线,以及通用公式vi和vii的类固醇衍生物,用于合成去甲酮地诺酮和依诺地诺酮.
专利号:US-9422326-B2 优先权日:2012-09-04 标 题:Process for preparing 11-methylene-18-methyl-estr-4-en-3, 17-dione, useful as intermediate compound for the synthesis of molecules having pharmacological activity 发明人:LENNA ROBERTO; MARIANI EDOARDO; VANOSSI ANDREA 权利人:IND CHIMICA SRL 摘要:There is described a process for the industrial synthesis of 11-methylene-18-methyl-estr-4-en-3,17-dione, a compound having the structure formula (I) depicted below: (Formula I) (I) useful as intermediate compound in the synthesis of the progestin compounds Desogestrel and Etonogestrel.
专利号:US-9464108-B2 优先权日:2012-03-15 标 题:Combined synthesis route for desogestrel and etonogestrel 发明人:OSTENDORF MARTIN 权利人:MSD OSS BV; MERCK SHARP & DOHME 摘要:The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.
专利号:WO-2004101594-A1 优先权日:2003-05-14 标题 :New mono-and bismethylene-steroid derivatives and process for their synthesis 发明人:TUBA ZOLTAN; DANCSI LAJOSNE; FRANCSICSNE CZINEGE ERZSEBET; FALKAY GYOERGY; ZUPKO ISTVAN; MARKI ARPAD; MOLNAR CSABA; CSOERGEI JANOS; DUKATNE ABROK VILMA; BALOGH GABOR; MAK MARIANNA 权利人:RICHTER GEDEON VEGYESZET; TUBA ZOLTAN; DANCSI LAJOSNE; FRANCSICSNE CZINEGE ERZSEBET; FALKAY GYOERGY; ZUPKO ISTVAN; MARKI ARPAD; MOLNAR CSABA; CSOERGEI JANOS; DUKATNE ABROK VILMA; BALOGH GABOR; MAK MARIANNA 摘要:The invention relates to new mono- and bismethylene-steroid derivatives of general formula (I) - wherein Z represents two hydrogen atoms or an oxo group; X and Y independently of each other represent either two hydrogen atoms of a CH2= group, with the restriction that at least one of them is CH2= group and if the meaning of Z is oxo group Y represents two hydrogen atoms, R represents a C1-C4 alkyl group, as well as the pharmaceutical compositions containing the above compounds as active ingredients, and the processes for the synthesis of active ingredients and pharmaceutical compositions. The invention also relates to the methods of treatments with these compounds, which means administering to a mammal to be treated with progestogen - including human - effective amount/amounts of the active ingredients of the present invention as such or as medicament. The mono- and bismethylene-steroid derivatives of the general formula (I) have progestogen effect. They can be used as active ingredients of contraceptive medicaments as such or in combination with an estrogen component. Furthermore, they can be used in the treatment of endometriosis and in the substitution therapy of estrogen as gestagen agent beside the estrogen component. The mono- and bismethylene-steroid derivatives of the general formula (I) of the present invention can be synthesized by reacting a compound of the general formula (II), - wherein the meaning of Z, X and Y is as described for the compounds of formula (I) - with an acid anhydride of the general formula (R-CO)2O or with an acid chloride of the general formula R-CO-Cl - wherein R represents a C1-C4 alkyl group - in the presence of a strong acid.
专利号:US-2013123523-A1 优先权日:2011-11-10 标 题:Methods for the preparation of etonogestrel and desogestrel 发明人:NICKISCH KLAUS; SANTHAMMA BINDU 权利人:NICKISCH KLAUS; SANTHAMMA BINDU 摘要:Described herein is a process for the synthesis of etonogestrel and desogestrel and intermediates used to form etonogestrel and desogestrel.
专利号:US-7667056-B2 优先权日:2002-08-02 标 题 :Process and new intermediates for the preparation of steroids with a progestogen activity 发明人:GRISENTI PARIDE; PECORA FABIO; VERZA ELISA; LEONI MASSIMO; BOSSI LAURA 权利人:POLI IND CHIMICA SPA 摘要:The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).
专利号:US-2008234340-A1 优先权日:2007-03-09 标 题:Synthesis and characterization of polymorph form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-YL)thiazol-4-YL)benzonitrile 发明人:MIRMEHRABI MAHMOUD; NIU YUPING; TADAYON ABDOLSAMAD; DESHMUKH SUBODH; KU MANNCHING SHERRY 权利人:WYETH CORP 摘要:A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. n Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
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合成参考文献
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