(6Alpha,9Beta,11Beta,16Alpha)-9,11-环氧-6-氟-17,21-二羟基-16-甲基-孕甾-1,4-二烯-3,20-二酮置于氢氟酸体系中,化学反应 5.0H,反应生成氟米松 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-7208613-B2 优先权日:2002-06-20 标 题:Synthesis of s-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate 发明人:JADAV KANAKSINH JESINGBHAI; KAMBHAMPATI SUDHAKAR; CHITTURI TRINADHA RAO; THENNATI RAJAMANNAR 权利人:SUN PHARMACEUTICAL IND LTD 摘要:The present invention provides a convenient process for the preparation of S-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate, a compound of formula 1, comprisingn (a) treating 17β-[(N,N-dimethylcarbamoyl)thio]carbonyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene, a compound of formula 3 with alkali metal carbonate-alcohol system to obtain 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioic acid, a compound of formula 4; (b) reacting the compound of formula 4 with bromofluoromethane to yield the compound of formula 1.
专利号:US-10954265-B2 优先权日:2016-10-14 标 题 :Structures and mechanism for the design of highly potent glucocorticoids 发明人:XU HUAQIANG ERIC; HE YUANZHENG 权利人:VAN ANDEL RES INSTITUTE 摘要:The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
专利号:US-9975918-B2 优先权日:2013-09-25 标 题:Highly potent glucocorticoids 发明人:XU HUAQIANG ERIC; HE YUANZHENG; MELCHER KARSTEN; YI WEI; SHI JINGJING 权利人:VAN ANDEL RES INSTITUTE; SHANGHAI INST MATERIA MEDICA CAS 摘要:The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
专利号:US-2005256325-A1 优先权日:2002-06-20 标题:Convenient synthesis of s-fluoromethyl 6alpha, 9alpha-difluoro-11beta-hydroxy-16alpha-methyl-17alpha-propionyloxy-3-oxoandrosta-1,4-diene-17beta-carbothioate
1: Jiang Y, Li W, Deng S, Li Q, Liu W, Ye H, Liang J, Zhang X. Flumethasone- salicylic acid cream effectively flattened verrucous epidermal nevus: a case report. J Dermatolog Treat. 2026 Dec;37(1):2603129. doi: 10.1080/09546634.2025.2603129. Epub 2025 Dec 29. 380:994-1004. doi: 10.1016/j.jconrel.2025.02.046. Epub 2025 Feb 22. 47(6):867-877. doi: 10.1080/03639045.2021.1908341. Epub 2021 Jul 5. 474:94-105. doi: 10.1016/j.canlet.2020.01.010. Epub 2020 Jan 16.
合成参考文献
参考文献:10.1177/1087057116635503 摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.