3-氨基-1-丙醇 以95%的收率获得1,3-丙二胺 参考文献:Process For The Preparation Of Amines 标题:Process For The Preparation Of Amines 摘要:描述了一种用于制备主要脂肪族聚胺的单级过程,其化学式为其中r1和r2彼此独立地是氢,甲基,乙基或氨甲基,通过在co/ni催化剂上在氢气存在下与超临界氨反应的多元醇.
专利信息
专利号:WO-0206209-A1 优先权日:2000-07-19 标 题 :Synthesis method for n1,n3-bis (2.aminoethyl) propane-1,3-diamine, synthesis intermediates, resulting products and use thereof in synthesis of cyclam 发明人:HANDEL HENRI; BERNARD HELENE; ANTOINE MARINE 权利人:UNIV BRETAGNE OCCIDENTALE; HANDEL HENRI; BERNARD HELENE; ANTOINE MARINE 摘要:The invention concerns a method of synthesis of a linear polynitrogen-containing derivative, namely N1,N3-bis (2-aminoethyl) propane-1,3-diamine of general formula (I) using as synthesis intermediates compounds (II) and (III). The invention also concerns the resulting products and their use in the synthesis of cyclic polynitrogen-containing derivatives such as cyclam.
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:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-2006293466-A1 优先权日:2003-06-20 标 题:Methods for synthesis of graft polymers 发明人:GAUTHIER MARIO; YUAN ZHONGSHUN 权利人:UNIV WATERLOO 摘要:A process for the synthesis of arborescent polymers comprises epoxidation of a first polymer and grafting thereto a second polymer having groups reactive to the epoxide groups on the first polymer. The epoxidation and grafting steps can be repeated. In an additional embodiment, the present invention provides a one-pot method for the synthesis of arborescent polymers. In a reaction pot, a first polymer is copolymerized and then reacted with an activating compound in order to generate a polyfunctional macroinitiator. Monomers are then added to the reaction pot, the monomers having functional groups reactive towards reactive sites on the first polymer.
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.
参考文献:10.1021/ic901620e 摘要:Fester GW, Eckstein J, Gerlach D, Wagler J, Brendler E, Kroke E. Reactions of hydridochlorosilanes with 2,2'-bipyridine and 1,10-phenanthroline: complexation versus dismutation and metal-catalyst-free 1,4-hydrosilylation. Inorg Chem. 2010 Mar 15;49(6):2667–73. doi: 10.1021/ic901620e. 参考文献:10.1107/s1600536811008324 摘要:Meer AF, Ahmad S, Sharif S, Khan IU, Ng SW. catena-Poly[bis(propane-1,3-diaminium) [[aqua(sulfato-κO)bis(sulfato-κ2O,O′)cerate(IV)]-μ-sulfato-κ3O,O′:O′′] dihydrate]. Acta Crystallogr E Struct Rep Online. 2011 Mar 09;67(4):m413. doi: 10.1107/s1600536811008324. 参考文献:10.1107/s1600536811009287 摘要:Aghabozorg H, Foroughian M, Foroumadi A, Bruno G, Amiri Rudbari H. N1,N1-Dimethylpropane-1,2-diaminium bis(6-carboxypyridine-2-carboxylate) monohydrate. Acta Crystallogr E Struct Rep Online. 2011 Mar 19;67(4):o932–3. doi: 10.1107/s1600536811009287. 参考文献:10.1111/j.1365-2958.2011.07757.x 摘要:Green R, Hanfrey CC, Elliott KA, McCloskey DE, Wang X, Kanugula S, Pegg AE, Michael AJ. Independent evolutionary origins of functional polyamine biosynthetic enzyme fusions catalysingde novodiamine to triamine formation. Molecular Microbiology. 2011 Jul 18;81(4):1109–24. doi: 10.1111/j.1365-2958.2011.07757.x. 参考文献:10.1021/ja205547h 摘要:Campbell R, Cannon D, García-Álvarez P, Kennedy AR, Mulvey RE, Robertson SD, Sassmannshausen J, Tuttle T. Main group multiple C-H/N-H bond activation of a diamine and isolation of a molecular dilithium zincate hydride: experimental and DFT evidence for alkali metal-zinc synergistic effects. J Am Chem Soc. 2011 Aug 31;133(34):13706–17.