专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-3876705-A 优先权日:1972-06-12 标 题:Steroid total synthesis and intermediates 发明人:VALENTA ZDENEK 权利人:UNIV NEW BRUNSWICK 摘要:A new steroidal synthesis process is described wherein the steroidal nucleus is provided by a Diels-Alder reaction between a 2,6-lower alkylbenzoquinone and a suitably substituted 1-vinylnaphthalene compound. Depending on the nature of the naphthalene compound it is possible to readily prepare estrones, progesterones, androstanes and cortisones having the natural configuration or if desired having the retro configuration.
专利号:US-3920748-A 优先权日:1972-06-12 标题:Steroid total synthesis and intermediates 发明人:VALENTA ZDENEK 权利人:HOFFMANN LA ROCHE 摘要:A new steroidal synthesis process is described wherein the steroidal nucleus is provided by a Diels-Alder reaction between a 2,6-lower alkylbenzoquinone and a suitably substituted 1-vinylnaphthalene compound. Depending on the nature of the naphthalene compound it is possible to readily prepare estrones, progesterones, androstanes and cortisones having the natural configuration or if desired having the retro configuration.
专利号:US-8362286-B2 优先权日:2009-08-13 标题:Method for making 3α-hydroxy, 3β- substituted-5α-pregnan-20-ones 发明人:SHAW KENNETH; HUTCHISON ALAN 权利人:MARINUS PHARMACEUTICALS INC; SHAW KENNETH; HUTCHISON ALAN 摘要:Applicants have discovered a method for the stereoselective and regioselective synthesis of 3α-hydroxy, 3β-methyl-5α-pregnan-20-one (ganaxolone) comprising reacting 5α-pregnane-3,20-dione; with an organometallic methylating agent in an inert solvent to provide a compound of the formula
专利号:US-3040091-A 优先权日:1961-03-15 标 题 :Process for synthesis of steroids and compounds thereof 发明人:WEISENBORN FRANK L 权利人:OLIN MATHIESON
专利号:US-2977286-A 优先权日:1959-05-22 标 题:Synthesis of steroids with kabatiella phoradendri 发明人:LASKIN ALLEN I; GUIDUCCI MARIANO A; JOSEF FRIED 权利人:OLIN MATHIESON
1: Conley AJ, Scholtz EL, Legacki EL, Corbin CJ, Knych HK, Dujovne GD, Ball BA, Moeller BC, Stanley SD. 5α-dihydroprogesterone concentrations and synthesis in non-pregnant mares. J Endocrinol. 2018 Jul;238(1):25-32. doi: 10.1530/JOE-18-0215. 146:132-136. doi: 10.1016/j.eplepsyres.2018.07.022. Epub 2018 Jul 29. 155(3):251-258. doi: 10.1530/REP-17-0380. Epub 2018 Jan 16. 149:27-34. doi: 10.1016/j.jsbmb.2015.01.004. Epub 2015 Jan 13. 158(6):R197-R208. doi: 10.1530/REP-19-0179. 231(1):23-33. doi: 10.1530/JOE-16-0175. Epub 2016 Jul 27.
合成参考文献
摘要:Journal of Medicinal Chemistry., 11(117), 1968 摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要:Ruskin, J.; Lectka, T., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2. 参考文献:10.1210/jc.81.10.3644|10.1210/jcem.81.10.8855816 摘要:Chantilis S, Dombroski R, Shackleton CH, Casey ML, MacDonald PC. Metabolism of 5 alpha-dihydroprogesterone in women and men: 3 beta- and 3 alpha-,6 alpha-dihydroxy-5 alpha-pregnan-20-ones are major urinary metabolites. The Journal of Clinical Endocrinology & Metabolism. 1996 Oct;81(10):3644–9. doi: 10.1210/jcem.81.10.8855816. 参考文献:10.1530/jrf.0.1070241 摘要:Schutzer WE, Kerby JL, Holtan DW. Differential effect of trilostane on the progestin milieu in the pregnant mare. J Reprod Fertil. 1996 Jul;107(2):241–8. doi: 10.1530/jrf.0.1070241.