间苯二甲腈 反应生成1,3-环己二甲胺 参考文献:Method Of Conveying Liquids 标题:Method Of Conveying Liquids 摘要:本发明涉及一种连续输送化学反应中用作起始物料的液体的方法,该方法采用位移泵,该泵具有物理上分离的正向输送阀和液体填充的双向流动管路,其中在双向流动管路中存在一种辅助液体,该液体是化学反应的产物或起始物料,并且其熔点低于被输送的液体的熔点或饱和温度. 本发明还提供了将芳香化合物氢化生成的产物用作辅助液体输送芳香化合物的用途,以及将醇或由醇和羧酸衍生的酯用作辅助液体输送羧酸或羧酸衍生物的用途.
专利信息
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: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-2010191010-A1 优先权日:2007-07-02 标题 :Process for the synthesis of carbamates using co2 发明人:BOSMAN JORIS KAREL PETER; CARR ROBERT HENRY 权利人:HUNTSMAN INT LLC 摘要:Process for the synthesis of non cyclic carbamate derivatives from amine compounds, alcohols and CO 2 in the presence of ionic liquids and optionally in the presence of a base.
专利号:US-5416189-A 优先权日:1992-11-04 标 题:Process for the synthesis of polyamides 发明人:VANDEVIJVER ERIC; GAUTHY FERNAND; MOMTAZ ARDECHIR 权利人:SOLVAY 摘要:Process for the synthesis of polyamides by polycondensation in a closed reactor of one or a number of dicarboxylic acids with a diamine compound containing not less than 60 mol % of-m-xylyenediamine, in which all the amount of diamine compound stoichiometrically necessary for the polycondensation reaction is quickly brought into contact with the molten acid, the temperature of the reaction mixture is raised to a value greater than the melting point of the polyamide produced, the pressure is only allowed to rise to a value sufficient to prevent solidification of the reaction mixture and a substantial loss of diamine compound and, at the end of the reaction, the pressure of the reaction mixture is reduced and the polyamide formed is recovered.
参考标题:Design And Synthesis Of A Library Of Tertiary Amides: Evaluation As Mimetics Of The Melanocortins' Active Core 作者:Felikss Mutulis,Jana Kreicberga,Sviatlana Yahorava,Ilze Mutule,Larisa Borisova-Jan,Aleh Yahorau,Ruta Muceniece,Sandra Azena,Santa Veiksina,Ramona Petrovska |发布日期:2007.9.1 摘要:Acceptable Results. According To This Approach An Efficient Formation Of Schiff Bases Was Achieved In The Presence Of Ticl(4). Substances Were Isolated By Reversed Phase Chromatography; In Some Cases Isomers Were Additionally Separated By Chiral Chromatography On Chirobiotic T. When Tested On Human Recombinant Melanocortin Receptors All The Tertiary Amides Showed Some Binding Affinities; For The Highest Affinity