专利号:US-4764263-A 优先权日:1987-05-18 标 题:Electrochemical synthesis of substituted aromatic amines in basic media 发明人:GREGORY THOMAS D; STUTTS KENNETH J 权利人:DOW CHEMICAL CO 摘要:Substituted amino aromatic compounds such as 3-amino-4-hydroxybenzoic acid are prepared by electrolytically reducing the corresponding nitro aromatic compound in a basic medium at temperatures below 60° C. and current densities greater than 50 milliamps per square centimeter. The aminohydroxybenzoic acids are useful in the preparation of polybenzoxazoles which are used to make fibers and composites having high strength and thermal stability.
专利号:WO-9729091-A1 优先权日:1996-02-09 标题:Balanol analogues 发明人:NIELSEN JOHN; LYNGSOE LARS OLE 权利人:AUDA PHARMACEUTICALS APS; NIELSEN JOHN; LYNGSOE LARS OLE 摘要:The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.
专利号:US-4603209-A 优先权日:1984-09-07 标题 :Fluorescent indicator dyes for calcium ions 发明人:TSIEN ROGER Y; GRYNKIEWICZ GRZEGORZ 权利人:UNIV CALIFORNIA 摘要:The present invention discloses a new class of highly fluorescent indicator dyes that are specific for calcium ions. The new fluorescent indicator dyes combine a stilbene-type fluorophore with a tetracarboxylate parent Ca 2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of EGTA and BAPTA. Preferred forms contain extra heterocyclic bridges to reinforce the ethylenic bond of the stilbene and to reduce hydrophobicity. Compared to their widely used predecessor, 'quin2', the new dyes offer up to thirty-fold brighter fluorescence, major changes in wavelength (not just intensity) upon Ca 2+ binding, slightly lower affinities for Ca 2+ , slightly longer wavelengths of excitation, and considerably improved selectivity for Ca 2+ over other divalent cations. These properties, particularly the wavelength sensitivity to Ca 2+ , make the dyes useful indicators for many intracellular applications, especially in single cells, adherent cell layers, or bulk tissues. n The present invention also discloses an improved method for synthesizing alpha-acyloxyalkyl bromides wherein the bromides so synthesized are free of contaminating bis(1-bromoalkyl)ether. The improved method is exemplified herein in the synthesis of acetoxymethyl bromide, a compound useful in preparing the acetoxymethyl esters disclosed herein as novel Ca 2+ specific fluorescent indicators.
专利号:WO-8809398-A1 优先权日:1987-05-18 标 题:Electrochemical synthesis of substituted amines in basic media
专利号:EP-0291865-A2 优先权日:1987-05-18 标 题:Electrochemical synthesis of substituted aromatic amines in basic media
专利号:FI-86563-C 优先权日:1987-05-18 标题:Electrochemical synthesis of substituted amines in basic media
参考标题:Fe/s-Catalyzed Synthesis Of 2-Benzoylbenzoxazoles And 2-Quinolylbenzoxazoles Via Redox Condensation Of O-Nitrophenols With Acetophenones And Methylquinolines 作者:Le Anh Nguyen,Thi Thu Tram Nguyen,Quoc Anh Ngo,Thanh Binh Nguyen 摘要:An Fe/s Catalyst Generated In Situ From Fecl2.4H2O And Elemental Sulfur S8 In The Presence Of A Tertiary Amine As A Base Was Found To Catalyze Efficiently A 6E− Redox Condensation Of O-Nitrophenols With Acetophenones And Methylquinolines. The Condensed Products 2-Benzoylbenzoxazoles And 2-Quinolylbenzoxazoles Were Obtained In Reasonable Yields With Water As The Only Byproduct At A Temperature As Low
合成参考文献
摘要:R. A. Robinson and A. Peiperl, J. Phys. Chem. 67, 1723 (1963). 摘要:C. K. Hancock and A. D. H. Clague, J. Am. Chem. Soc. 86, 4942 (1964).