📜(6Alpha,9Beta,11Beta,16Alpha)-9,11-环氧-6-氟-17,21-二羟基-16-甲基-孕甾-1,4-二烯-3,20-二酮置于盐酸,4-二甲氨基吡啶,碘代三甲硅烷,异丙醇体系中,用 二氯甲烷,水,乙腈 用作溶剂,化学反应 5.25H,反应生成氯可托龙 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-8802660-B2 优先权日:2007-03-12 标 题:De novo synthesis of glucocorticoids in the epidermis and its uses and applications 发明人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H 权利人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H; UNIV NEW YORK 摘要:The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.
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.
1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Clocortolone Pivalate. 2021 Jan 18. 12(2):s3-4. 72(2):161-6. 5:61-8. doi: 10.2147/CCID.S23227. Epub 2012 Jun 22. 5: Nierman MM. Safety and efficacy of clocortolone pivalate 0.1 percent cream in the treatment of atopic dermatitis, contact dermatitis, and seborrheic dermatitis. Cutis. 1981 Jun;27(6):670-1. 5(7):20-4.