CAS: 356-12-7; Fluocinolone Acetonide Acetate

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CAS号67-73-2 醋酸氟轻松 | CAS号108-24-7 乙酸酐 | CAS号3932-49-8 21-O-acetyl 1,2... | CAS号67-73-2 醋酸氟轻松

醋酸阿奈可他置于吡啶,Potassium Permanganate,甲酸,高氯酸,乙酸异丙烯酯,葡萄糖,N,N-二甲基乙酰胺,氢氟酸,Potassium Acetate,对甲苯磺酸体系中,用 甲醇,Aq. Phosphate Buffer,水,N,N-二甲基甲酰胺,丙酮,乙腈 作为反应溶剂,化学反应 35.0H,反应生成 醋酸氟轻松
参考文献:氟轻松的改进合成及6α,9α-氟化反应工艺研究
标题:氟轻松的改进合成及6α,9α-氟化反应工艺研究
摘要:从 21-乙酰氧基-17α-羟基-4,9(11)-二烯-3,20-二酮 (1A) 开发了一种高效,改进的氟轻松与生物发酵相结合的合成路线.研究了 6α 和 9α 氟化步骤的过程,观测到 6α 氟化的立体选择性高度依赖于底物.在对氟化试剂和活化试剂进行广泛筛选后,6α-F 以 85% 的收率和 98.9% 的立体选择性引入.代替 Hf 气体,在 9α 氟化步骤中应用 Hf 水溶液,以 89% 的收率提供所需的产物.从 1A 开始,氟轻松分 9 个步骤制备,总产率为 38.5%.
DOI:10.1246/cl.170923

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-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-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.