CAS: 2607-06-9; Diflucortolone

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CAS号2135-17-3 氟米松 | CAS号4571-51-1 9β,11β-epoxy-6α... | CAS号23961-95-7 9beta,11beta-ep...

📜9Beta,11Beta-环氧-6Alpha-氟-17,21-二羟基-16Alpha-甲基孕甾-1,4-二烯-3,20-二酮 21-乙酸酯置于碘代三甲硅烷,氢氟酸,水,Potassium Carbonate体系中,用 甲醇,乙腈 用作溶剂,化学反应 17.0H,反应生成双氟可龙
参考文献: Process For The Preparation Of 17-Desoxy-Corticosteroids[fr] Procédé De Préparation De 17-Désoxy-Corticostéroïdes
标题: Process For The Preparation Of 17-Desoxy-Corticosteroids[fr] Procédé De Préparation De 17-Désoxy-Corticostéroïdes
摘要:本发明提供了一种改进的方法,通过将17-羟基起始物与过量的碘化三甲基硅烷反应,在单一化学步骤中制备17-去氧皮质类固醇衍生物.本发明在制备具有卤素基团的17-去氧皮质类固醇衍生物方面具有明显优势,这些卤素基团位于皮质类固醇的2,6,7或9位,例如氯科尔酮或去氧美他松.

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-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:EP-1422235-B1
优先权日:2001-07-26
标题 :Stereoselective method of producing 6alpha-fluoropregnanes and intermediaries
发明人：MURILLO GARRIDO JOSE VICENTE; SILVA GUISASOLA LUIS OCTAVIO; MARTIN JUAREZ JORGE
权利人:RAGACTIVES SL
摘要:6 alpha -fluorpregnanes (I), where the dotted line between positions 1 and 2 represents a single or double bond; R1 is OH, OCOR2, X, SO3R3, or an (R7)(R8)(R9)SiO- group, where X is halogen, R2 and R3 are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, and R7, R8 and R9, equal or different, are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, can be obtained by means of a high stereoselectivity process comprising reacting a 3-(trisubstituted)silyloxy-pregna-3,5-diene (IV) with a fluorinating agent selected among N-fluorosulfonimides and N-fluorosulfonamides. The 6 alpha -fluorpregnanes (I) are intermediates for the synthesis of steroids useful as anti-inflammatory and anti-asthmatic agents.

专利号:WO-9709067-A1
优先权日:1995-09-05
标 题 :Combination of 5-lipoxygenase and leukotriene synthesis inhibitors with glucocorticosteroids
发明人：BURCHARDT ELMAR-REINHOLD; MUELLER-PEDDINGHAUS REINER
权利人:BAYER AG; BURCHARDT ELMAR REINHOLD; MUELLER PEDDINGHAUS REINER
摘要:The combination is disclosed of 5-lipoxygenase inhibitors as direct action lipoxygenase inhibitors (LOI) or of leukotriene synthesis inhibitors (LSI) with glucocorticosteroids (GCS). This combination is suitable for treating and preventing various acute and chronic inflammatory processes, in particular of the respiratory tract, and may therefore be used as a medicament, in particular for treating asthma.