3-(Tert-Butyl)-1-(4-Methoxybenzyl)-5,5-Diphenylimidazolidine-2,4-Dione置于甲烷磺酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 24.0H,以72%的收率获得产物苯妥英 参考文献:Palladium Catalyzed C-Arylation Of Amino Acid Derived Hydantoins 标题:Palladium Catalyzed C-Arylation Of Amino Acid Derived Hydantoins 摘要:Palladium(II) Trifluoroacetate (5 Mol %) Catalyzes The C-Arylation Of N,N-Disubstituted Hydantoins By Aryl Iodides In Good Yield. The Reaction Proceeds Through Base-Promoted Enolization Of The Amino Acid Derived Hydantoins,And The Resulting 5,5-Disubstituted Hydantoins May Be Deprotected At One Or Both N Atoms To Yield Biologically Active Structures Or Alternatively Hydrolyzed To The Parent A-Aryl A-Amino Acids. The Reaction Is Successful With A Variety Of Parent Amino Acids And A Range Of Electron-Rich And Electron-Poor Aryl Iodides. DOI:10.1021/acs.Orglett.5B01803
专利号:US-6376667-B1 优先权日:1997-11-26 标 题 :Solid phase synthesis of heterocycles 发明人:CASTELHANO ARLINDO L; SHAO HUI 权利人:OSI PHARM INC 摘要:Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.
专利号:US-9662347-B2 优先权日:2010-05-11 标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system 发明人:LEE BONG HEE; BYUN KYUNG HEE 权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND 摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.
专利号:WO-2025133656-A1 优先权日:2023-12-21 标题 :Synthesis and use of tuned precatalyst for carbon-monoxide and carbon-dioxide based fischer-tropsch catalyst for controlled product distribution 发明人:SÃ?PI ANDRÃ?S; NAJARI SARA; KÓNYA ZOLTÃ?N; KUKOVECZ Ã?KOS; SAEIDE SAMRAND 权利人:UNIV SZEGEDI 摘要:The present invention belongs to the technical field of design and synthesis of carbon-monoxide and carbon-dioxide-based Fischer-Tropsch synthesis catalysts, and discloses a novel iron-based Fischer-Tropsch synthesis catalyst containing both iron and carbon and a synthesis method and use thereof. The present invention specifically relates to a catalyst mixture for use in hydrogenation of CO and/or CO2, which catalyst mixture comprises i) iron oxide promoted by alkali metal, alkaline earth metal or transition metal, and ii) iron carbide. The invention further relates to a method for production of iron carbide composite comprising different iron carbides, and the use of said carbide composite in combination with alkali metal, alkaline earth metal or transition metal promoted iron oxide for use in hydrogenation of CO and/or CO2.
专利号:US-5714127-A 优先权日:1992-10-08 标题 :System for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J 权利人:WARNER LAMBERT CO 摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.
专利号:WO-02061120-A1 优先权日:2001-02-01 标题:Method of evaluating ability of drug to induce enzyme in liver cells 发明人:OHTA KUNIHIRO; NAKAGAWA TOSHITO 权利人:CHUGAI PHARMACEUTICAL CO LTD; OHTA KUNIHIRO; NAKAGAWA TOSHITO 摘要:A method of evaluating the ability of a test drug to induce the synthesis of CYP (cytochrome P450) in liver cells characterized by comprising culturing the liver cells in a culture medium containing the test drug in the presence of matrigel and evaluating the ability of the test drug to induce the synthesis of CYP by assaying the enzymatic activity of CYP in the culture medium.
专利号:US-5702672-A 优先权日:1992-10-08 标 题 :Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KELL MICHAEL; PAVIA MICHAEL R; KIELY JOHN S; SCHROEDER MEL C; STANKOVIC CHARLES J; WARE STEVEN 权利人:WARNER LAMBERT CO 摘要:An apparatus for multiple, simultaneous synthesis of compounds which consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.
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