5'-羟基-2',5',7'-三甲基螺[环丙烷-1,6'-茚]-4'-酮 (-)-Acylfulvene 125392-76-9 隐陡头菌素; 隐杯伞素; 月亮霉素 Illudin S 1149-99-1
合成工艺路线路线简述
📜隐陡头菌素; 隐杯伞素; 月亮霉素置于硫酸体系中,用 四氢呋喃 用作溶剂,化学反应 48.0H,反应生成(-)-伊洛福芬 参考文献:Synthesis Of [3H]-Illudin S,[3H]-Acylfulvene,[3H] & [14C]-Hydroxymethylacylfulvene (Mgi 114) 标题:Synthesis Of [3H]-Illudin S,[3H]-Acylfulvene,[3H] & [14C]-Hydroxymethylacylfulvene (Mgi 114) 摘要:Tritiated Derivatives Of The Toxic Sesquiterpene Illudin S (1) Have Been Prepared By Fermentation Of Omphalotus Illudens In The Presence Of [h-3]-Sodium Acetate. [h-3]-Illudin S Was Converted To Antitumor [h-3]-Acylfulvene (4) By Treatment With Dilute Sulfuric Acid. Antitumor [c-14]-Hydroxymethylacylfulvene (5) Was Best Prepared By Reacting Acylfulvene With [c-14]-Paraformaldehyde In Dilute Sulfuric Acid. Doi:10.1002/(Sici)1099-1344(199804)41:4<279::Aid-Jlcr86>3.0.Co;2-J
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:US-2024352049-A1 优先权日:2023-04-19 标 题:Direct synthesis of alkoxysilanes using copper-aluminum alloy catalysts 发明人:LEWIS KENRICK MARTIN; MEREIGH ABELLARD 权利人:MOMENTIVE PERFORMANCE MAT INC 摘要:An improved catalyzed reaction of silicon metal with alcohol is provided for the formation of alkoxysilanes, particularly trialkoxysilanes. The Direct Synthesis reaction of silicon metal and alcohol employs a catalytically effective amount of a copper-aluminum alloy as a catalyst precursor and further benefits from an effective catalyst-promoting amount of a catalyst promoter.
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-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-8598153-B2 优先权日:2006-09-22 标题 :Method of treatment using fatty acid synthesis inhibitors 发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN 权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME 摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.
1: Staake MD, Kashinatham A, McMorris TC, Estes LA, Kelner MJ. Hydroxyurea derivatives of irofulven with improved antitumor efficacy. Bioorg Med Chem Lett. 2016 Apr 1;26(7):1836-8. doi: 10.1016/j.bmcl.2016.02.028. Epub 2016 Feb 13. doi: 10.1016/j.ajhg.2014.01.007. 3: Glatt H, Pietsch KE, Sturla SJ, Meinl W. Sulfotransferase-independent genotoxicity of illudin S and its acylfulvene derivatives in bacterial and mammalian cells. Arch Toxicol. 2014 Jan;88(1):161-9. doi: 10.1007/s00204-013-1097-2. Epub 2013 Jul 24. doi: 10.1124/jpet.112.195768. Epub 2012 Aug 15. 5: Schilder RJ, Blessing JA, Shahin MS, Miller DS, Tewari KS, Muller CY, Warshal DP, McMeekin S, Rotmensch J. A phase 2 evaluation of irofulven as second-line treatment of recurrent or persistent intermediately platinum-sensitive ovarian or primary peritoneal cancer: a Gynecologic Oncology Group trial. Int J Gynecol Cancer. 2010 Oct;20(7):1137-41.
合成参考文献
摘要:Lee, D.; O'Connor, M., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 1, 99. 摘要:Fundamental and Applied Toxicology., 36(1 参考文献:10.1021/np960450y 摘要:McMorris TC, Kelner MJ, Wang W, Yu J, Estes LA, Taetle R. (Hydroxymethyl)acylfulvene: an illudin derivative with superior antitumor properties. J Nat Prod. 1996 Sep;59(9):896–9. doi: 10.1021/np960450y. 参考文献:10.1007/s004320050299 摘要:Matsuura H, Schuller DE, Fukushima M, Coltman Jr CA. Summary of the proceedings of the United States and Japan Head and Neck Cancer Clinical Trials Summit, 19-20 September 1997, Kyoto, Japan. Journal of Cancer Research and Clinical Oncology. 1999 Jun 02;125(7):433–8. doi: 10.1007/s004320050299. 参考文献:10.1016/s0968-0896(99)00016-4 摘要:McMorris TC. Discovery and development of sesquiterpenoid derived hydroxymethylacylfulvene: a new anticancer drug. Bioorganic & Medicinal Chemistry. 1999 May;7(5):881–6. doi: 10.1016/s0968-0896(99)00016-4.