CAS: 152-43-2; (8R,9S,13S,14S,17R)-3-(Cyclopentyloxy)-17-Ethynyl-13-Methyl-7,8,9,11,12,13,14,15,16,17-Decahydro-6H-Cyclopenta[a]Phenanthren-17-Ol

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CAS号96-41-3 环戊醇 | CAS号100271-25-8 3,3-ethanediyld... | CAS号124263-27-0 3,3-ethanediyld...

19-Acetoxyandrosta-1,4-Diene-3,17-Dione置于正丁基锂,三氟甲磺酸体系中,用 四氢呋喃,异丙醇 用作溶剂,化学反应 4.0H,反应生成炔雌醇环戊醚
参考文献:3-醚化雌酮的环保合成
标题:3-醚化雌酮的环保合成
摘要:常规醚化使用有毒或难降解的烷基化剂.提出了一种生态友好的串联醚化/芳香化反应,以从容易获得的二烯酮1制备雌酮3-仲醚.用该方法从市售的起始原料合成了三种市售的3-醚化雌激素药物.
Doi:10.1016/j.Tet.2016.03.002

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-6093805-A
优先权日:1991-01-22
标 题:Glycoside compounds and methods of synthesis
发明人：SHULL BRIAN K; TUINMAN ROELAND J; HOUSTON TODD A; KLEMKE R ERICH; KOREEDA MASATO
权利人:UNIV MICHIGAN
摘要:Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.

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:WO-2024097977-A1
优先权日:2022-11-04
标题:Silk nanoparticle synthesis: tuning size, dispersity, and surface chemistry for drug delivery
发明人：SHAIDANI SAWNAZ; FALCUCCI THOMAS; FOSTER OLIVIA; SAHOO JUGAL KISHORE; HASTURK ONUR; KAPLAN DAVID L; JACOBUS CHARLOTTE S
权利人:TUFTS COLLEGE
摘要:Methods disclosed herein relate to generating silk nanoparticles with a low polydispersity index (PDI). Methods include adding a silk solution dropwise into a volatile solvent that is miscible with water, thereby forming a precipitate-bearing solution and applying shear forces to the precipitate-bearing solution for a length of time sufficient to achieve evaporation of at least 95% of the volatile solvent, thereby producing a population of silk fibroin nanoparticles in water having a polydispersity index (PDI) of 0.35 or less, including but not limited to, a PDI of 0.330 or less, 0.325 or less, 0.315 or less, 0.310 or less, 0.30 or less, 0.275 or less, 0.250 or less, 0.225 or less, or 0.200 or less. Parameters related to silk fibroin molecular weight, silk fibroin concentration, shear force application, and temperature may all be modified to achieve silk nanoparticles of a particular size exhibiting particular PDIs.

专利号:US-2005070715-A1
优先权日:2003-07-15
标 题:Methods for synthesis of acyloxyalkyl compounds