CAS: 17721-06-1; Thiophen-3-Amine

上下游产品

CAS号872-31-1 3-溴噻吩 | CAS号22288-78-4 3-氨基-2-噻吩甲酸甲酯 | CAS号82685-95-8 N-thienyl-3 car... | CAS号10486-61-0 3-碘噻吩 | CAS号55341-87-2 3-氨基-2-噻吩甲酸 | CAS号106-39-8 对氯溴苯 | CAS号1210469-45-6 potassium 3-ami... | CAS号1003-04-9 四氢噻吩-3-酮 | CAS号78756-27-1 3-氨基噻吩-2-羧酸钠 | CAS号106944-13-2 2-溴噻吩-3-胺 | CAS号42602-67-5 N-(3-噻吩基)乙酰胺 | CAS号19228-91-2 N-B°C-3-氨基噻吩 | CAS号74695-44-6 5,7-二氯噻吩并[3,2-b]吡啶 | CAS号116538-95-5 (9CI)-噻吩并[3,2-b... | CAS号65076-02-0 2-((噻吩-3-基氨基)亚甲... | CAS号913377-45-4 2,2-Dimethyl-5-... | CAS号61528-50-5 3-异硫氰基噻吩

3-碘噻吩置于ammonium Hydroxide,Potassium Phosphate,8-(2-Methyl-1-Propanone)-5,6,7,8-Tetrahydroquinoline,Copper(I) Bromide体系中,用 二甲基亚砜 用作溶剂,化学反应 24.0H,以80%的收率获得3-氨基噻吩
参考文献:氨水对铜进行芳烃卤化物的高效铜催化胺化
标题:氨水对铜进行芳烃卤化物的高效铜催化胺化
摘要:溴化铜(i)/ 1-(5,6,7,8-四氢喹啉-8-基)-2-甲基丙烷-1-酮(cubr-L3)的组合催化了芳基卤化物或杂芳基卤化物与在室温或温和条件下高产氨水以生产伯芳族或杂芳族胺.
Doi:10.1002/adsc.200900327

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-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-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.

专利号:US-2005119332-A1
优先权日:1998-03-12
标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases)
发明人：JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU
摘要:The present invention provides novel compounds of formula 1a, n nnovel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

专利号:WO-9946244-A1
优先权日:1998-03-12
标题 :Modulators of protein tyrosine phosphatases (ptpases)
发明人：JEPPESEN LONE; ANDERSEN HENRIK SUNE; OLSEN OLE HVILSTED; JUDGE LUKE MILBURN; HOLSWORTH DANIEL DALE; BAKIR FARID; AXE FRANK URBAN; GE YU
权利人:NOVO NORDISK AS; ONTOGEN CORP
摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.