CAS: 616-46-6; Thiophen-2-Amine

上下游产品

CAS号56267-50-6 N-(2-噻吩基)氨基甲酸叔丁酯 | CAS号3437-95-4 2-碘噻吩 | CAS号1003-09-4 2-溴噻吩 | CAS号609-40-5 2-硝基噻吩 | CAS号372-09-8 氰基乙酸 | CAS号4471-47-0 formyl cyanide | CAS号120-92-3 环戊酮 | CAS号7439-89-6 铁粉 | CAS号592489-23-1 1,3-dimethyl-2-... | CAS号527-72-0 2-噻吩甲酸 | CAS号100037-80-7 6-phenylthieno[... | CAS号56267-50-6 N-(2-噻吩基)氨基甲酸叔丁酯 | CAS号13362-81-7 (6CI,7CI,8CI,9C... | CAS号136-34-5 Benzamide, N-2-... | CAS号65075-97-0 ethyl 2-cyano-3... | CAS号59713-52-9 diethyl 2-[(thi... | CAS号61528-56-1 O-propyl N-thio...

📜2-溴噻吩置于c24H32N2*clcu,氨,Potassium Carbonate体系中,用 N-甲基吡咯烷酮,甲醇 作为反应溶剂,90.0 °C,689.49 Kpa 条件下,反应 24.0H,以88%的收率获得产物噻吩胺
参考文献:使用铜-卡宾催化剂将芳基/杂芳基溴化物与氨进行交叉偶联.
标题:使用铜-卡宾催化剂将芳基/杂芳基溴化物与氨进行交叉偶联.
摘要:在铜-Nhc催化剂的存在下,将各种芳基和杂芳基溴化物与氨以非常好或高收率交联.
DOI:10.1039/b815757J

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: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-6117992-A
优先权日:1996-08-26
标题 :Reagents and process for synthesis of oligonucleotides containing phosphorodithioate internucleoside linkages
发明人：IYER RADHAKRISHNAN P
权利人:HYBRIDON INC
摘要:The invention provides new methods for synthesizing oligonucleotides containing at least one, and preferably all phosphorodithioate internucleoside linkages with less than 5% phosphoromonothioate contamination. This level of purity in the synthesis of phosphorodithoates has previously been very difficult to achieve with all existing methods. The invention further provides phosphorothioamidite nucleoside synthons comprising a sulfur protecting group that is stable under normal oligonucleotide synthesis conditions.

专利号:US-7781488-B2
优先权日:2002-06-10
标 题:Post-cleavage sulfur deprotection for convergent protein synthesis by chemical ligation
发明人：BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT
权利人:AMYLIN PHARMACEUTICALS INC
摘要:The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.

专利号:US-8178474-B1
优先权日:1999-04-21
标题 :Functionalised solid support for alpha-oxoaldehyde synthesis
发明人：MELNYK OLEG; FRUCHART JEAN-SEBASTIEN; BOUREL LINE; GRAS-MASSE HELENE
权利人:MELNYK OLEG; FRUCHART JEAN-SEBASTIEN; BOUREL LINE; GRAS-MASSE HELENE; PASTEUR INSTITUT; CENTRE NAT RECH SCIENT
摘要:The invention relates to a functionalised solid support for the synthesis of compounds comprising at least one α-oxoaldehyde function, to a process for preparing it and to its applications, in particular for the preparation of a library of organic compounds, of a diagnostic reagent, of a microtitration plate and of a biochip, such as a DNA chip. The present invention also relates to a process for the synthesis of organic compounds comprising at least one α-oxoaldehyde function and to the α-oxoaldehyde peptides obtained using this process.

专利号:US-6310180-B1
优先权日:1993-06-21
标 题 :Method for synthesis of proteins
发明人：TAM JAMES P
权利人:UNIV VANDERBILT
摘要:A method for peptide synthesis is disclosed that requires neither protecting groups nor activation of the C-α carboxyl groups. The method comprises ligating a first molecule to a second molecule by promoting the orthogonal coupling of the molecules to each other. In an aspect of this method, an acyl-type reaction occurs between the molecules. The method contemplates the joining of molecules of variant size to each other, as well as the coupling of multiple identical molecules. The invention also covers the ligation of unprotected peptide, proteins or nonpeptide segments to prepare therapeutic products and synthetic vaccines with linear, circularized, or branched backbone structures, as well as the site-specific modification of peptides or proteins by lipidation and pegylation.