CAS: 61951-99-3; 11β,17α-Dihydroxy-21-Mercapto-4-Pregnene-3,20-Dione

📜S-(2-((8S,9S,10R,11S,13S,14S,17R)-11,17-Dihydroxy-10,13-Dimethyl-3-Oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-1H-Cyclopenta[a]Phenanthren-17-yl)-2-Oxoethyl) Benzothioate置于sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 0.5H,反应生成 替可的松
参考文献:Expeditious Synthesis Of Steroids Containing A 2-Methylsulfanyl-Acetyl Side Chain As Potential Glucocorticoid Receptor Imaging Agents
标题:Expeditious Synthesis Of Steroids Containing A 2-Methylsulfanyl-Acetyl Side Chain As Potential Glucocorticoid Receptor Imaging Agents
摘要:In Our Effort To Develop Imaging Agents For Brain Glucocorticoid Receptors,We Have Prepared Several Novel Glucocorticoids Possessing A 2-Methylsulfanyl-Acetyl Side Chain. The Synthesis Was Accomplished Via A Mitsunobu Reaction With Thiobenzoic Acid Starting From Cortisol,Prednisolone,Dexamethasone And Triamcinolone Acetonide To Give The Corresponding S-Thiobenzoates In 75-82% Yield. Subsequent Saponification And Reaction With Methyl Iodide Afforded C-21 Methylthioethers In 68-82% Yield. All Compounds Were Tested In An In Vitro Glucocorticoid Receptor-Binding Assay. Triamcinolone Acetonide-Based Compound 12 Showed Promising Binding Affinity Of 144% Relative To Dexamethasone (100%). Compound 12 Was Selected For Radiolabeling With The Short-Lived Positron Emitter Carbon-11. The Radiolabeling Was Carried Out Starting From S-Thiobenzoate 8 And In Situ Formation Of The Corresponding Sodium Thiolate,Which Was Further Reacted With [c-11]Methyl Iodide. The Obtained Radiochemical Yield Was 20-30%. The Specific Activity Was Determined To Be 20-40 Gbq/mu Mol At The End-Of-Synthesis,And The Radiochemical Purity Exceeded 98%. (C) 2007 Elsevier Inc. All Rights Reserved
DOI:10.1016/j.Steroids.2007.08.013

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: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:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:US-9994558-B2
优先权日:2013-09-20
标题 :Multicyclic compounds and methods of using same
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

专利号:US-8697730-B2
优先权日:2007-10-26
标题 :5-lipoxygenase activating protein (FLAP) inhibitor
发明人：REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON
权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC
摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.