CAS: 1247-42-3; (8S,9S,10R,13S,14S,16S,17R)-17-Hydroxy-17-(2-Hydroxyacetyl)-10,13,16-Trimethyl-7,8,9,10,12,13,14,15,16,17-Decahydro-3H-Cyclopenta[a]Phenanthrene-3,11(6H)-Dione

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CAS号1106-03-2 16-甲基泼尼松醋酸酯

16,17A-Epoxy Prednisone置于对甲苯磺酸,乙二胺,原甲酸三乙酯体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应生成甲基泼尼松
参考文献:甲基泼尼松的制备方法
标题:甲基泼尼松的制备方法
摘要:甲基泼尼松的制备方法,是将由4‑雄烯二酮(简称4Ad)制备的16(17)A‑环氧泼尼松在有机溶剂中与乙二醇在10‑50oc酸催化反应得缩酮物:20‑缩酮基‑16(17)A‑环氧泼尼松;再将缩酮物在有机溶剂中与三甲基氯硅烷碱催化反应得硅醚物:21‑甲硅醚基‑20‑缩酮基‑16(17)A‑环氧泼尼松;再将硅醚物在有机溶剂中与2M甲基卤化镁进行格氏反应,所得格氏物在强酸中水解制得甲基泼尼松,检测得HPLC含量99.0%以上,熔点228‑237°C,合成重量总收率80‑85%.以本发明生产甲基泼尼松,原料来源广泛,工艺经济环保,生产操作简便,合成路线短,合成收率高,生产成本比传统方法低30‑40%;利于工业化生产.

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:WO-2022226312-A1
优先权日:2021-04-22
标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
发明人：KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
权利人:CLEAR CREEK BIO INC
摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

专利号:US-9573873-B2
优先权日:2014-06-03
标题:Catalytic method for dibenzocycloheptane synthesis and allocolchicinoid synthesis
发明人：GREEN JAMES; MEHDI MARIAM; DJURDJEVIC SINISA
权利人:UNIV OF WINDSOR
摘要:In a non-limiting embodiment, there is provided a compound of formula (I), which may permit for a method or use in treating or preventing a cancer, such as pancreatic cancer or leukemia. In one embodiment, there is also provide a method of preparing a compound of formula (Ia), the method including conducting a cyclization reaction of a compound of formula (III) to obtain a compound of formula (IV), wherein conducting the cyclization reaction comprises conducting a Michael reaction in the presence of a Lewis acid.

专利号:US-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

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.