CAS: 434-03-7; (8R,9S,10R,13S,14S,17R)-17-Ethynyl-17-Hydroxy-10,13-Dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-3H-Cyclopenta[a]Phenanthren-3-One

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CAS号20380-17-0 21-bromo-17α-hy... | CAS号63-05-8 雄烯二酮 | CAS号74-86-2 乙炔 | CAS号3604-60-2 Pregn-5-en-20-y... | CAS号24594-68-1 3-ethoxy-17α-et... | CAS号1971-59-1 18-Norandrosta-... | CAS号976-71-6 坎利酮 | CAS号1096-38-4 16-去氢黄体酮 | CAS号604-09-1 17alpha-羟基黄体酮 | CAS号640-87-9 孕甾-4-烯-17α,21-二... | CAS号33784-05-3 7β-螺内酯 | CAS号1235-98-9 Pregna-4,20-die... | CAS号52-01-7 螺内酯 | CAS号145430-54-2 17-(2-iodoethyn...

雄烯二酮置于硫酸,对甲苯磺酸,Potassium Hydroxide体系中,用 四氢呋喃,乙醇 作为反应溶剂,化学反应 17.5H,反应生成 炔孕酮
参考文献:达那唑的制备方法
标题:达那唑的制备方法
摘要:本发明公开了一种达那唑及其中间体的制备方法,它是以雄甾烯二酮为起始原料,经3位烯醇醚化,17位羰基乙炔化,3位水解化,2位次甲羟化以及肟化制得达那唑.3位烯醇醚化是先由雄甾烯二酮与原甲酸三乙酯在无水乙醇以及对甲苯磺酸的存在下,在30~50oc的温度下反应4~10H;然后再在0~10oc的温度下加入三乙胺继续反应0.2~1H;17位羰基乙炔化是先将氢氧化钾粉在乙炔气流中,在5~10oc的温度下反应1~2H;然后再与3位烯醇醚化产物在四氢呋喃以及催化剂的存在下,在15~30oc的温度下在乙炔气流中反应2~4H.本发明的3位烯醇醚化反应条件温和,收率较高,而17位羰基乙炔化反应收率较高,时间也较短.

专利信息

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人：GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

专利号:US-4041055-A
优先权日:1975-11-17
标题:Process for the preparation of 17α-hydroxyprogesterones and corticoids from androstenes
发明人：SHEPHARD KENNETH PAUL; VAN RHEENEN VERLAN H
权利人:UPJOHN CO
摘要:This invention discloses a general process for the production of corticoids from androstenes. This invention provides an economically viable alternative synthesis of 17α-hydroxyprogesterones and the corticoids.

专利号:US-6110906-A
优先权日:1989-03-10
标题:Androgen derivatives for use in the inhibition of sex steroid activity
发明人：LABRIE FERNAND; MERAND YVES
权利人:ENDORECHERCHE INC
摘要:Methods for treating sex steroid-dependent diseases by inhibiting sex steroid activity include administration of novel compounds which include an androgenic nucleus substituted at a ring carbon with at least one substituent specified herein. Such compounds may function by inhibiting sex steroid synthesis (both estrogen and androgen synthesis) and/or by antagonistically blocking androgen receptors.

专利号:US-2005239725-A1
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof

专利号:US-9056129-B2
优先权日:2007-02-09
标 题 :Precision-guided nanoparticle systems for drug delivery
发明人：HANSON ROBERT N; AMIJI MANSOOR; WEISSIG VOLKMAR
权利人:HANSON ROBERT N; AMIJI MANSOOR; WEISSIG VOLKMAR; UNIV NORTHEASTERN
摘要:A method of preparing multifunctionalized nanoparticles involves using a modular system of half-linkers to attach functional moieties that serve to deliver the nanoparticles to a desired target, exert an effect at the target, or track the nanoparticles within a cell or an animal. The modular chemistry of the half-linker system permits the custom design and synthesis of functionalized nanoparticles bearing multiple groups and therefore results in precise delivery to desired cell types and intracellular locations. The functionalized nanoparticles can be used to treat or diagnose a variety of medical conditions, including neoplastic diseases, infectious diseases, and chronic diseases.