专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-6051704-A 优先权日:1996-07-22 标题:Synthesis of macrocyclic tetraamido-N ligands 发明人:GORDON-WYLIE SCOTT W; COLLINS TERRENCE J 权利人:UNIV CARNEGIE MELLON 摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.
专利号:US-6011152-A 优先权日:1996-07-22 标 题 :Synthesis of macrocyclic tetraamido-N ligands
专利号:US-5191088-A 优先权日:1991-03-11 标题 :Aromatic monoanhydride-esters 发明人:BLYAKHMAN YEFIM 权利人:CIBA GEIGY CORP 摘要:Aromatic monoanhydride-esters of the formula (I) ##STR1## wherein R 1 is ##STR2## and R 2 is hydrogen, C 1 -C 4 alkyl or --OCH 3 are useful as endcapping agents for the synthesis of multifunctional high temperature resins such as polyimides, polyimide-esters, polyimide-ethers and polyimide-amides.
专利号:EP-0504109-A1 优先权日:1991-03-11 标题:Aromatic monoanhydride-esters 发明人:BLYAKHMAN YEFIM 权利人:CIBA GEIGY AG 摘要:Aromatic monoanhydride-esters of the formula (I)n n wherein R¹ isn n and R² is hydrogen, Câ‚?-Câ‚„alkyl or -OCH₃ are useful as endcapping agents for the synthesis of multifunctional high temperature resins such as polyimides, polyimide-esters, polyimide-ethers and polyimide-amides.
专利号:WO-2004076425-A1 优先权日:2003-02-21 标题:Improved synthesis of macrocyclic tetraamido compounds and new metal insertion process
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合成参考文献
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