📜(5Alpha)-雄甾烷-17-酮置于sodium Ethanolate体系中,化学反应生成 5-Alpha-雄烷 参考文献:Burrows Et Al.,Biochemical Journal,1937,Vol. 31,P. 950,957 标题:Burrows Et Al.,Biochemical Journal,1937,Vol. 31,P. 950,957
专利信息
专利号:US-4219489-A 优先权日:1978-09-05 标题:Synthesis of steroids 发明人:BUNES LEONARD A; JOHNSON WILLIAM S 权利人:STANFORD LELAND JUNIOR UNIV TR 摘要:Method and compounds are provided for use in the synthesis of steroids wherein a polyolefin is provided having an initiating group having a chalcogen atom in juxtaposition to a double bond, so as to be capable of bond formation to close to form a ring and having a terminating group involving pi unsaturation (a double or triple bond) conjugated to an aromatic ring. Upon acid catalysis, sigma bonds are formed through the interaction of a carbocation formed at the carbon atom bonded to the chalcogen atom and the double bond intermediate the initiating group and the terminating group, which close to form rings of a steroid nucleus, the carbocation interacting with the pi unsaturation conjugated with the aromatic group and being captured by a nucleophile present in the acidic reaction medium. The resulting steroid product may then be modified in known ways to produce known steroids.
专利号:US-7935837-B2 优先权日:2008-04-30 标 题:Process for synthesis of androstane 17-β carbothioic acid and relative compounds thereof 发明人:HSU NAI-HSUAN; PANG CHU-YI; WU CHIEN-JEN; HUANG CHI-JEN; HSU CHIA-JUNG; LEE PEIMIN 权利人:CORUM INC 摘要:A process for synthesis of androstane 17-β carbothioic acid is provided. The process includes mixing an androstane 17-β carboxylic acid and a coupling reagent, and adding an alkanethioic acid to form an androstane 17-β carbothioic acid, wherein the androstane 17-β carbothioic acid has the formula (I): n n n n n n n n n n n n wherein R 1 represents hydrogen or haloalkyl groups, R 2 represents C 1-8 linear alkyl groups, C 1-8 branched alkyl groups, C 1-6 unsaturated acyclic groups or aromatic groups, R 3 represents hydrogen or hydroxyl, R 4 represents hydrogen, bromine, chlorine or fluorine and R 5 represents hydrogen, bromine, chlorine or fluorine. The process is a one-pot reaction.
专利号:US-8367394-B2 优先权日:2007-07-04 标题:Process for the synthesis of 9α-hydroxy-steroids 发明人:OLASZ KATALIN; TEGDES ANIKO; GANCSOS VALERIA; HANTOS GABOR; KOENCZOEL KALMAN; BALOGH GABOR; ERDELYI SANDOR 权利人:RICHTER GEDEON NYRT; OLASZ KATALIN; TEGDES ANIKO; GANCSOS VALERIA; HANTOS GABOR; KOENCZOEL KALMAN; BALOGH GABOR; ERDELYI SANDOR 摘要:The present invention relates to a novel selective synthesis of 9α-hydroxy-steroid derivatives of the general formula (I) (I)—wherein the meaning of -A-A′- is —CH 2 —CH 2 — or —CHâ•?CH— group—by the bioconversion of compounds of the general formula (II) (II) wherein the meaning of -A-A′- is —CH 2 —CH 2 — or —CHâ•?CH— group—by using Nocardia farcinica bacterium strain, deposition number of which is NCAIM (P)—B 001342, as hydroxylating microorganism in the bioconversion.
专利号:WO-2013001322-A1 优先权日:2011-06-30 标 题:PROCESS FOR THE SYNTHESIS OF (5α,17β)-N-[(2,5-BIS(TRIFLUOROMETHYL)-PHENYL]-3-OXO-4-AZA-5-ANDROST-1-ENE-17-CARBOXAMIDE 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES 权利人:RICHTER GEDEON NYRT; SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES 摘要:The synthesis consists of reaction steps as follows: oxidizing the α,β-unsaturated ketone system of ring 'A' of pregn-4-ene-3,20-dion- of formula (II) with sodium metaperiodate in tert-butanol in the presence of potassium permanganate and alkali metal carbonate, reacting the obtained 3,5-seco acid with an ester of chloroformic acid in the presence of tertier organic base below 0°C, reacting the obtained new compound after isolation or without isolation with ammonia or ammonium acetate, cyclization of the resulting carboxamides with an acid, cathalytic hydrogenating the obtained ene lactame, and oxidizing the side chain at position 17 of the obtained pregnane compound with an alkali metal hypobromide in aqueous dioxane below 10°C. Thereafter on one hand the obtained (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is reacted with chloroformic acid ester, the obtained new compound is reacted with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acid, the obtained amide is reacted with trimethyl chlorosilane in inert atmosphere in the presence of Î?,Î?,Î?',Î?'-tetramethyl-ethylendiamine, then en excess iodine is added to the reaction mixture and the product of the iodination reaction is crystallized from acetonitrile, then the obtained 2-iodo-3-oxo-4-aza-17β-carboxamide is reacted with potassium tert-butylate to furnish final product. On the other hand, (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is transformed into methylester by known method, this latter is transformed into methyl (2α,5α,17β)-2-iodo-3-oxo-4-aza-5-androstane-17-carboxylate according to known method, the obtained compound is reacted with potassium-tert-butylate, the obtained (5α,17β)-3-oxo-4-aza-5-androst-1-ene-17-carboxylic acid is reacted with an ester of chloroformic acid, then the obtained new compound is coupled with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acidcatalyst to gain final product.
专利号:US-3772366-A 优先权日:1964-09-29 标 题 :Process for the preparation of 9beta,10beta steroids 发明人:USKOKOVIC M; WILLIAMS T 权利人:HOFFMANN LA ROCHE 摘要:THE PRESENT INVENTION IS DIRECTED TO A PROCESS FOR THE COMPLETE CHEMICAL SYNTHESIS OF STEROIDS HAVING THE 9B, 10A-CONFIGURATION FROM THE NATURAL STERIOIDS POSSESSING THE 9A, 10B-CONFIGURATION INCLUDING INTERMEDIATES IN THIS SYNTHESIS. THE STEROIDS WITH THE 9B,10A-CONFIGURATION ARE USEFUL AS ANABOLIC AGENTS, ANTI-ANDROGENIC AGENTS, PROGESTATIONAL AGENTS AND AS SALT-RETAINING AGENTS.
专利号:EP-0296097-B1 优先权日:1987-06-16 标 题:Medicine containing inhibitors of the progesterone synthesis of the trilostane or epostane type and antigestagens 摘要:The medicine contains a progesterone synthesis inhibitor (ProH) of the trilostane or epostane type and an antigestagen (AG) and is used for inducing labour at term in humans and animals and for terminating normal or pathological pregnancy. The combination according to the invention is also suitable for treating hormone-dependent tumours, endometriosis and dysmenorrhoea.
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 参考文献:10.1037/0735-7044.120.3.632 摘要:Pérez-Acevedo NL, Lathroum L, Jorge JC. The neurosteroid 3alphaDIOL modulates place preference when infused in the basolateral amygdala according to sex. Behav Neurosci. 2006 Jun;120(3):632–40. doi: 10.1037/0735-7044.120.3.632. 参考文献:10.1038/srep42037 摘要:Ye H, Yang Z, Wu X, Wang J, Du D, Cai J, Lv K, Chen H, Mei J, Chen M, Du H. Sediment biomarker, bacterial community characterization of high arsenic aquifers in Jianghan Plain, China. Scientific Reports. 2017 Feb 06;7(1):42037. doi: 10.1038/srep42037. 参考文献:10.1007/s12035-018-1085-x 摘要:Ludwig B, Roy B, Dwivedi Y. Role of HPA and the HPG Axis Interaction in Testosterone-Mediated Learned Helpless Behavior. Molecular Neurobiology. 2018 Apr 28;56(1):394–405. doi: 10.1007/s12035-018-1085-x. 参考文献:10.1016/j.exer.2005.10.021 摘要:Agapova OA, Kaufman PL, Hernandez MR. Androgen receptor and NFkB expression in human normal and glaucomatous optic nerve head astrocytes in vitro and in experimental glaucoma. Exp Eye Res. 2006 Jun;82(6):1053–9. doi: 10.1016/j.exer.2005.10.021.