合成目标产物 Fluticasone Propionate 主要起始原料 Bromofluoromethane And Fluticasone Propionate Intermediate
80473-92-3 + 373-52-4 = 80474-14-2 反应条件:1.1 Reagents: Triethylamine Solvents: Acetone; 0 °C; 1 H,0 °C1.2 Reagents: Diethylamine1.3 0 °C 标题:Improved Synthesis Of Fluticasone Propionate 作者:Yin,Limei; Et Al 参考文献:Zhongguo Yaowu Huaxue Zazhi 日期:2010 卷标:20(1) 页码:29-31]
80486-69-7 = 80474-14-2 反应条件:1.1 Reagents: Potassium Iodide Solvents: Acetone; 7 D,Reflux 标题:Synthesis Of Fluticasone Propionate 作者:Liu,Jin-Xian; Et Al 参考文献:Huaxi Yaoxue Zazhi 日期:2007 卷标:22(1) 页码:51-53]
192191-49-4 = 80474-14-2 反应条件:1.1 Reagents: Urea,Hydrofluoric Acid; -10 °C -> 15 °C1.2 Reagents: Ammonium Hydroxide Solvents: Water 标题:Process For Preparing Fluticasone Propionate 参考文献:Mexico]
373-53-5 + 65429-42-7 = 80474-14-2 反应条件:1.1 Reagents: Cesium Carbonate Solvents: Acetonitrile; Rt; 6 H,Rt1.2 Reagents: Water 标题:Direct And Chemoselective Electrophilic Monofluoromethylation Of Heteroatoms (O-,S-,N-,P-,Se-) With Fluoroiodomethane 作者:Senatore,Raffaele; Et Al 参考文献:Organic Letters 日期:2020 卷标:22(4) 页码:1345-1349
氟替卡松丙酸酯中间体置于4-二甲氨基吡啶,二氟代氙,氨,三乙胺,三氟乙酸体系中,用 四氢呋喃,甲醇,二氯甲烷 作为反应溶剂,化学反应 53.08H,反应生成 氟替卡松丙酸酯 参考文献:Method For The Production Of Fluoromethyl Esters Of Androstan-17 Beta Carboxylic Acids 标题:Method For The Production Of Fluoromethyl Esters Of Androstan-17 Beta Carboxylic Acids 摘要:本文描述了从保护中间体和/或试剂出发制备单氟甲基有机生物活性化合物的过程,以获得如丙酸氟替卡松和富马酸氟替卡松等化合物,其中使用脱羧试剂xef2和brf3或使用fch2Sh作为试剂.
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-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-11311505-B2 优先权日:2017-02-24 标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts 发明人:MARTIN ALAIN 权利人:MARTIN ALAIN; CELLULAR SCIENCES INC 摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
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合成参考文献
参考文献:10.1272/jnms.77.21 摘要:Nonaka M, Sakanushi A, Kusama K, Ogihara N, Yagi T. One-year evaluation of combined treatment with an intranasal corticosteroid and montelukast for chronic rhinosinusitis associated with asthma. J Nippon Med Sch. 2010 Feb;77(1):21–8. doi: 10.1272/jnms.77.21. 参考文献:10.1186/2047-783x-14-s4-104 摘要:Holownia A, Mroz R, Kielek A, Chyczewska E, Braszko J. Nuclear HSP90 and HSP70 in COPD patients treated with formoterol or formoterol and corticosteroids. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):104. doi: 10.1186/2047-783x-14-s4-104. 参考文献:10.1186/1471-2466-11-40 摘要:Müller V, Gálffy G, Eszes N, Losonczy G, Bizzi A, Nicolini G, Chrystyn H, Tamási L. Asthma control in patients receiving inhaled corticosteroid and long-acting beta2-agonist fixed combinations. A real-life study comparing dry powder inhalers and a pressurized metered dose inhaler extrafine formulation. BMC Pulmonary Medicine. 2011 Jul 15;11(1):40. doi: 10.1186/1471-2466-11-40.