专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6136984-A 优先权日:1996-04-22 标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-9410004-B2 优先权日:2008-05-21 标 题 :Aromatic polyethersulfone microparticles having narrow particle diameter distribution index 发明人:ASANO ITARU; ECHIGO YUJI; TAKEZAKI HIROSHI 权利人:TORAY INDUSTRIES 摘要:A fine polymer particle production method includes producing an emulsion in a liquid prepared by dissolving and mixing a polymer A and a polymer B in organic solvents in which a solution phase composed primarily of the polymer A and a solution phase composed primarily of the polymer B are formed as separate phases, and bringing it into contact with a poor solvent for the polymer A to precipitate the polymer A. This method serves for easy synthesis of fine polymer particles with a narrow particle size distribution and the method can be effectively applied to production of highly heat-resistant polymers that have been difficult to produce with the conventional methods.
专利号:CN-119100919-A 优先权日:2024-09-04 标 题:Preparation method of anhydrous rare earth acetate raw material and application of anhydrous rare earth acetate raw material in synthesis of rare earth nano luminescent material
专利号:WO-9740034-A1 优先权日:1996-04-22 标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
专利号:US-9125843-B2 优先权日:2013-10-03 标 题 :Methods and compositions for improving the appearance of skin 发明人:PERNODET NADINE A; COLLINS DONALD F 权利人:PERNODET NADINE A; COLLINS DONALD F; ELC MAN LLC 摘要:A method for stimulating collagen synthesis in aging skin cells in need of treatment by topically applying a composition comprising at least one extract from Laminaria genus, at least one extract from the Narcissus genus, and at least one peptide that stimulates sirtuin 6 activity in the form of a peptide or a yeast extract where the peptide is component of the extract; and a treatment composition comprising at least one extract from Laminaria genus, at least one extract from the Narcissus genus; and at least one peptide that stimulates sirtuin 6 activity.
1: Kindrat I, Dreval K, Shpyleva S, Tryndyak V, de Conti A, Mudalige TK, Chen T, Erstenyuk AM, Beland FA, Pogribny IP. Effect of methapyrilene hydrochloride on hepatic intracellular iron metabolism in vivo and in vitro. Toxicol Lett. 2017 Nov 5;281:65-73. doi: 10.1016/j.toxlet.2017.09.011. Epub 2017 Sep 19. doi: 10.1016/j.mrgentox.2014.04.004. Epub 2014 Apr 24. doi: 10.1016/j.tiv.2013.09.022. Epub 2013 Oct 2. doi: 10.1016/j.etp.2013.07.001. Epub 2013 Jul 23. doi: 10.1007/s00204-012-0847-x. Epub 2012 Apr 8. doi: 10.1016/j.mrgentox.2011.07.006. Epub 2011 Jul 27. doi: 10.1021/tx100141d. Erratum in: Mutat Res 1995 Apr;342(3-4):197.
合成参考文献
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