专利号:US-2019292219-A1 优先权日:2018-03-26 标 题:Method of solid-state peptide synthesis using a novel polymeric support 发明人:JERABEK KAREL; HANKOVA LIBUSE; HOLUB LADISLAV; ZECCA MARCO; CENTOMO PAOLO; TROVO DANIELE; LEDER RICCARDO; BIONDI BARBARA 权利人:INST OF CHEMICAL PROCESS FUNDAMENTALS OF THE CAS V V I; UNIV DEGLI STUDI PADOVA 摘要:A method of solid-state synthesis of peptides that provides a polymeric solid-state synthesis support, attaches a first amino acid to said support to form the first amino acid molecule of the desired peptide chain, attaches additional amino acids to form the desired peptide chain, characterized in that the polymeric solid-state synthesis support is a styrenic polymer containing at least 50 mol % divinylbenzene monomer units, the styrenic polymer being functionalized with chloromethyl and/or benzyloxybenzyl alcohol and/or amino moieties, and having porosity 60-90% and medium pore diameter ranging from 10 to 80 nm. A functionalized styrenic polymer is claimed.
专利号:US-4753985-A 优先权日:1981-10-07 标题 :Synthesis of organic compounds using deformable gel in porous rigid support 发明人:ROSEVEAR ALAN; SHEPPARD ROBERT C 权利人:ATOMIC ENERGY AUTHORITY UK 摘要:The present invention relates to the synthesis of chemical compounds and more particularly to the synthesis of organic compounds, for example, peptides and oligonucleotides. n The invention provides a composite material for use in the synthesis of organic compounds comprising a support material and, supported on the support material, an organic compound synthesizing substance. n It is preferred that the organic compound synthesizing substance is a gel (e.g. a dimethylacrylamide co-polymer gel). n The invention also provides a method for preparing a composite material for use in the synthesis of organic compounds and a method for the synthesis of organic compounds.
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.
参考标题:Fmoc-Amox, A Suitable Reagent For The Introduction Of Fmoc 作者:Ashish Kumar,Anamika Sharma,Elvira Haimov,Ayman El-Faham,Beatriz G. De La Torre,Fernando Albericio |发布日期:2017.10.20 摘要:Synthesis Of Most Peptides Is Achieved Using Solid-Phase Peptide Synthesis Employing The Fmoc/tert-Butyl Strategy. However, The Introduction Of Fmoc In N-Unprotected Amino Acids Seems To Be Challenging Due To The Formation Of Dipeptides And Sometimes Tripeptides As Impurities And β-Alanyl Impurities When Fmoc-Osu Is Used As Well. Herein, We Report An Efficient And Successful Method Using Fmoc-Amox
合成参考文献
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