📜醋酸曲安奈德置于吡啶,Sodium Hydroxide体系中,用 甲醇,二氯甲烷 作为反应溶剂,化学反应生成 己曲安奈德 参考文献: Novel Process For Preparation Of Glucocorticoid Steroids[fr] Nouveau Procédé De Préparation De Stéroïdes De Type Glucocorticoïde 标题: Novel Process For Preparation Of Glucocorticoid Steroids[fr] Nouveau Procédé De Préparation De Stéroïdes De Type Glucocorticoïde 摘要:本发明揭示了一种制备16,17-孕烷衍生物的16,17-缩醛的方法,其具有式(I)的结构,其中每个取代基独立地选择自; R1为h或ch3; R2为c1-C6直链或支链烷基,炔基或环烷基; 芳基或杂环芳基; 或r1和r2结合形成饱和的,不饱和的c3-C6环或杂环环; R3和r4相同或不同,每个独立地表示h或卤素; R5为-Oh或-ocor,其中r表示h或c1-C6直链,支链或环烷基,可能被取代.
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-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-8926955-B2 优先权日:2008-12-22 标题 :Synthesis of polymer conjugates of indolocarbazole compounds 发明人:BAGNOD RAFFAELLA; BECCARIA LUCA; BERTARIONE RAVA ROSSA LUISA; CRISCUOLO DOMENICO; LORENZETTO CHIARA; MAINERO VALENTINA; MARCONI ALESSANDRA; PINCELLI CARLO; TRAVERSA SILVIO 权利人:BAGNOD RAFFAELLA; BECCARIA LUCA; BERTARIONE RAVA ROSSA LUISA; CRISCUOLO DOMENICO; LORENZETTO CHIARA; MAINERO VALENTINA; MARCONI ALESSANDRA; PINCELLI CARLO; TRAVERSA SILVIO; CREABILIS S A 摘要:The present invention relates to a process for the preparation of polymer conjugates of indolocarbaxole compounds, in particular of polymer conjugates of K-252a and derivatives thereof, by a synthetic route which results in a highly pure product, with a high product yield. In a further aspect the present invention relates to novel polymer conjugates of K-252a and derivatives thereof, wherein the chemical group linking the polymer unity to the K-252a or to the K-252a derivative compound is characterized by a 5-member oxazolidindionic cyclic structure. These novel polymer conjugates are obtained through the novel synthetic route with high purity and high yields.
专利号:WO-9925385-A1 优先权日:1997-11-17 标 题:A method of increasing nucleic acid synthesis with ultrasound 发明人:UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID 权利人:IMARX PHARMACEUTICAL CORP 摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.
专利号:WO-2025024697-A1 优先权日:2023-07-27 标 题:Intermediates for synthesizing exatecan mesylate 发明人:GOEDDEL DAVID; WALKER JAMES; WRIGHT AUSTIN; REDFERN LOUIS 权利人:SIGMA ALDRICH CO LLC 摘要:Intermediates useful in the preparation of exatecan mesylate and related compounds. Further provided are methods for preparing these compounds. Also provided is an improved, scalable synthesis of exatecan mesylate using the provided intermediates. The synthesis of exatecan mesylate utilizes a convergent approach, involving fewer steps and utilizing fewer reagents and increasing efficiency.
1: Sun W, Ho S, Fang XR, O'Shea T, Liu H. Simultaneous determination of triamcinolone hexacetonide and triamcinolone acetonide in rabbit plasma using a highly sensitive and selective UPLC-MS/MS method. J Pharm Biomed Anal. 2018 May 10;153:267-273. doi: 10.1016/j.jpba.2018.02.052. Epub 2018 Feb 23. doi: 10.1590/1806-9282.63.10.827. Review. doi: 10.1590/1413-785220172505172581. 4: McCormack R, Lamontagne M, Vannabouathong C, Deakon RT, Belzile EL. Comparison of the 3 Different Injection Techniques Used in a Randomized Controlled Study Evaluating a Cross-Linked Sodium Hyaluronate Combined With Triamcinolone Hexacetonide (Cingal) for Osteoarthritis of the Knee: A Subgroup Analysis. Clin Med Insights Arthritis Musculoskelet Disord. 2017 Aug 14;10:1179544117725026. doi: 10.1177/1179544117725026. eCollection 2017. 5: Resnick CM, Vakilian PM, Kaban LB, Peacock ZS. Is Intra-Articular Steroid Injection to the Temporomandibular Joint for Juvenile Idiopathic Arthritis More Effective and Efficient When Performed With Image Guidance? J Oral Maxillofac Surg. 2017 Apr;75(4):694-700. doi: 10.1016/j.joms.2016.09.045. Epub 2016 Oct 6. doi: 10.1590/1413-785220172502151116.
合成参考文献
参考文献:10.1002/art.21488 摘要:af Klint E, Grundtman C, Engström M, Catrina AI, Makrygiannakis D, Klareskog L, Andersson U, Ulfgren AK. Intraarticular glucocorticoid treatment reduces inflammation in synovial cell infiltrations more efficiently than in synovial blood vessels. Arthritis Rheum. 2005 Dec;52(12):3880–9. doi: 10.1002/art.21488.