专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-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-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles 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 under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-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-4801744-A 优先权日:1985-03-01 标 题 :Catalytic synthesis of urea from carbon monoxide and amine compound 发明人:HERMAN JEAN-JACQUES; LECLOUX ANDRE 权利人:SOLVAY 摘要:Process for the catalytic synthesis of nitrogen-containing organic compounds, comprising the reaction of carbon monoxide with at least one amino compound in a reaction mixture containing a catalyst based on selenium and a substituted pyridine. The process is particularly suitable for the synthesis of ureas and of their polymers.
专利号:WO-9961509-B1 优先权日:1998-05-21 标题:Synthesis of semi-crystalline polyphthalamides through reactive extrusion of hexamethylene terephthalamide oligomer with lower melting, semi-crystalline or amorphous polyamides 发明人:LEBOEUF CHRISTIAN; HARBOURNE DAVID ALAN 权利人:LEBOEUF CHRISTIAN; HARBOURNE DAVID ALAN 摘要:This invention relates to the synthesis of semi-crystalline polyphthalamides (i.e. containing monomeric units of terephthalic acid and hexamethylene diamine) through reactive extrusion of hexamethylene terephthalamide oligomer, or the oligomer of another 6T-rich copolymer, with lower melting semi-crystalline or amorphous polyamides. This process is particularly useful since it is centered around the use of stirred autoclaves for the synthesis of the 6T oligomer and the semi-crystalline or amorphous polyamides which are subsequently combined in a twin screw extruder equipped for devolatilization of water of reaction. It can also be used for the modification of existing semi-crystalline or amorphous polyamides (not necessarily phthalamides) with low levels of 6T.
专利号:WO-2023152730-A1 优先权日:2022-02-14 标题 :Amine-borane adducts in the synthesis of polyester and its copolymers using cyclic esters and compositions thereof 发明人:FENG XIAOSHUANG; LIU JINGJING; GNANOU YVES 权利人:UNIV KING ABDULLAH SCI & TECH 摘要:Embodiments of the present disclosure provide for the process of synthesis of polyester and its copolymers through (co)polymerization of cyclic esters and with other oxygenated monomers using amine-borane adduct. Embodiments of the present disclosure further describe the controlled anionic ring-opening polymerization of the cyclic compounds. Embodiments of the present disclosure also describe the polymerization of cyclic compounds using the synergistic effect of amines and thioureas. Embodiments of the present disclosure also describe compositions of polymers formed by the said process.
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合成参考文献
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