CAS: 1524-88-5; Flurandrenolide

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CAS号1526-01-8 6-α-氟-21-羟基-16α...

📜氟尼缩松置于wilkinson'S Catalyst,氢气体系中,用 乙醇,甲苯 用作溶剂,化学反应 65.0H,以76%的收率获得氟氢缩松
参考文献:6α-Fluoro-和 6α,9α-Difluoro-11β,21-Dihydroxy-16α,17α-Propylmethylenedioxypregn-4-Ene-3,20-Dione:合成和评价其 C-22 差向异构体的活性和动力学
标题:6α-Fluoro-和 6α,9α-Difluoro-11β,21-Dihydroxy-16α,17α-Propylmethylenedioxypregn-4-Ene-3,20-Dione:合成和评价其 C-22 差向异构体的活性和动力学
摘要:摘要 人们普遍认为,糖皮质激素的抗炎作用与其在受体水平上的不良反应是分不开的.然而,通过结构改变来改变药代动力学可以为类固醇提供比目前使用的更好的治疗指数.因此,合成并研究了丁醛和 6α-氟-或 6α,9α-二氟-16α-羟基皮质醇之间的新 16α,17α-缩醛.相应的 16α,17α-二醇的缩醛化或它们的 16α,17α-丙酮化物在二恶烷中的转缩醛化产生 C-22 差向异构体的混合物,这些混合物通过制备色谱法进行拆分.或者,通过在存在惰性材料的烃中进行缩醛化和转缩醛化,使用一种有效的方法立体选择性地生产 22R-差向异构体.(22R)-6α,9α-Difluoro-11β,21-Dihydroxy-16α,17α-Propylmethylenedioxypregn-4-Ene-3,20-Dione 的 C-22 构型通过单晶 X 射线衍射明确确定.本发明化合物,尤其是刚刚提到的22R-差
Doi:10.1016/s0039-128X(97)00107-4

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-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-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.