CAS: 51372-29-3; 7-Hydroxy-8B-(2-Hydroxyacetyl)-6A,8A-Dimethyl-10-Propyl-1,2,6A,6B,7,8,8A,8B,11A,12,12A,12B-Dodecahydro-4H-Naphtho[2',1':4,5]Indeno[1,2-D][1,3]Dioxol-4-One

该化合物是布德森ide(Budesonide)的立体异构体,一种具有强效抗炎和免疫抑制特性的合成甘蓝胶类动物,其特征是口服生物利用率低,而且快速的先行代谢,这进一步减少了不良效应.该化合物的稳定性和可预期的药性支持其在受控释放配方中的使用.其临床效用是有据可查的,特别是在吸入疗法中,它通过改进安全剖面来提供有针对性的抗炎效果.

结构式图片

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CAS号123-72-8 正丁醛 | CAS号638-94-8 地索奈德 | CAS号13951-70-7 16α-羟基泼尼松龙

合成工艺路线路线简述

    16Alpha-羟基泼尼松龙置于甲醇,高氯酸,三乙胺,Sodium Hydroxide体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 布地奈德
    参考文献:Cn115785188
    标题:Cn115785188

    海关参考信息

    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: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-10813893-B2
    优先权日:2017-02-24
    标 题:Compositions and methods for the treatment and prevention of chronic hypoxemia and dyspnea
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:The present invention has shown that not all salts of pyruvic acid enhance lung functions or enhance the synthesis of lung surfactants and that certain salts of pyruvic acid with the correct concentrations of calcium, phosphate and magnesium, are synergistic in their ability to enhance the synthesis of lung surfactants that will enhance lung alveoli functions, while decreasing coughing and lung tightness, and increasing oxygen saturation values to prevent hypoxemia. This patent demonstrates that the sodium pyruvate formula with calcium, phosphate and magnesium was superior over standard sodium pyruvate formula in saline alone in the removal of mucus, reduction of lung or sinus infections, and in reducing drug side effects and congestion. The use of this formula clearly demonstrated that it can be used to produce better efficacy in patients with hypoxemia, with lung and sinus diseases including, asthma, COPD, cystic fibrosis, interstitial lung disease, allergic rhinitis, sinusitis, Alzheimer's, disease, Parkinson's disease, brain trauma, nicotine addiction, sleep apnea, autism, migraine headaches, sleep disorders, lung and sinus infections, cancer therapy with cancer drugs, nicotine addiction, and medications that cause a decrease in lung surfactants.
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    合成参考文献


    参考文献:10.1007/s00216-010-3484-3
    摘要:Peters RJB, Oosterink JE, Stolker AAM, Georgakopoulos C, Nielen MWF. Generic sample preparation combined with high-resolution liquid chromatography–time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2583–98. doi: 10.1007/s00216-010-3484-3.
    参考文献:10.1111/j.1365-2982.2010.01472.x
    摘要:Walter SA, Münch A, Ost A, Ström M. Anorectal function in patients with collagenous colitis in active and clinically quiescent phase, in comparison with healthy controls. Neurogastroenterol Motil. 2010 May;22(5):534–8, e118. doi: 10.1111/j.1365-2982.2010.01472.x.
    参考文献:10.1186/2047-783x-14-s4-71
    摘要:Fischer A, Stegemann J, Scheuch G, Siekmeier R. Novel devices for individualized controlled inhalation can optimize aerosol therapy in efficacy, patient care and power of clinical trials. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):71. doi: 10.1186/2047-783x-14-s4-71.
    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:10.1186/2047-783x-14-s4-108
    摘要:Holownia A, Mroz RM, Kolodziejczyk A, Chyczewska E, Braszko JJ. Increased FKBP51 in induced sputum cells of chronic obstructive pulmonary disease patients after therapy. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):108. doi: 10.1186/2047-783x-14-s4-108.
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