L-(+)-Fmoc-鸟氨酸盐酸盐置于三乙胺,1,4-二巯基-2,3-丁二醇体系中,用 Aq. Phosphate Buffer,二氯甲烷,甲苯 用作溶剂,化学反应 12.08H,反应生成Fmoc-L-瓜氨酸 参考文献: Photocaged Citrulline Analogs And Methods For Site-Specific Incorporation Of Citrulline Into Proteins[fr] Analogues De Citrulline Photobloquée Et Procédés D'Incorporation De Citrulline Spécifique Au Site Dans Des Protéines 标题: Photocaged Citrulline Analogs And Methods For Site-Specific Incorporation Of Citrulline Into Proteins[fr] Analogues De Citrulline Photobloquée Et Procédés D'Incorporation De Citrulline Spécifique Au Site Dans Des Protéines 摘要:The Invention Provides Novel Compounds And Methods For Site-Specific Incorporation Of Citrulline Into Peptides And Proteins In Mammalian Cells. The Invention Also Relates To Modified Peptides And Proteins With Site Specific Citrullination And Pharmaceutical Compositions And Methods Of Preparation And Use Thereof.
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: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-12251674-B2 优先权日:2012-11-14 标 题:Substrates, systems, and methods for array synthesis and biomolecular analysis 发明人:RAJASEKARAN JOHN J; JAYARAMAN VASANTH; WANG TIANHAO; BEI KANG; KRISHNAMURTHY HARI KRISHNAN; VEDANTHAM PUNITHA 权利人:VIBRANT HOLDINGS LLC 摘要:Disclosed herein are formulations, substrates, and arrays. In certain embodiments, substrates and arrays comprise a porous layer for synthesis and attachment of polymers or biomolecules. Also disclosed herein are methods for manufacturing and using the formulations, substrates, and arrays, including porous arrays. Also disclosed herein are formulations and methods for one-step coupling, e.g., for synthesis of peptides in an N→C orientation. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate.
专利号:US-8410028-B2 优先权日:2003-12-17 标 题:Methods for synthesis of encoded libraries 发明人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A 权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC 摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
专利号:US-2024209034-A1 优先权日:2021-04-12 标题:Engineering peptides for a a vb6 integrin binding and related methods of use and synthesis 发明人:SELLERS DREW; CARDLE IAN; PUN SUZIE HWANG 权利人:UNIV WASHINGTON; SEATTLE CHILDRENS HOSPITAL D/B/A SEATTLE CHILDRENS RES INSTITUTE 摘要:Embodiments of the claimed invention are directed to synthetic peptides comprising an amino acid sequence of X 1 X 2 VX 3 NLRGDLQVLX 4 QKVCX 5 T (SEQ ID NO:18), wherein at least one of X 1 and X 2 is a cysteine, and wherein one or more of X 3 , X 4 , and X 5 is a non-natural amino acid. Also described are methods of using the claimed embodiments for inhibiting growth of a cancer cell overexpressing integrin αvβ6. Additionally, also described are methods of using the claimed embodiments for detecting a cancer cell overexpressing integrin αvβ6.