CAS: 5345-47-1; 2-Aminonicotinic Acid

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2-氯烟酸置于ammonium Hydroxide,2-O-Methyl-L-Inositol,Copper(II) Acetate Monohydrate体系中,用 N-甲基吡咯烷酮 作为反应溶剂,化学反应 12.0H,以72%的收率获得产物2-氨基烟酸
参考文献:Quebrachitol 或二甘醇促进的铜 (II)-催化芳基卤化物和 N-亲核试剂的 C-N 偶联
标题:Quebrachitol 或二甘醇促进的铜 (II)-催化芳基卤化物和 N-亲核试剂的 C-N 偶联
摘要:在本文中,我们报告了天然配体 Quebrachitol (Qct) 作为 Cu(II) 催化剂的促进剂,它对各种胺和相关芳基卤化物的 N-芳基化非常有效.通过使用二甘醇(deg)作为配体和溶剂,以高收率获得了一系列二芳胺衍生物.c-N偶联反应在温和的条件下进行并表现出非常好的官能团耐受性.
DOI:10.1055/s-0039-1690707

专利信息

专利号:US-6225329-B1
优先权日:1998-03-12
标 题 :Modulators of protein tyrosine phosphatases (PTPases)
发明人：RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN
权利人:NOVO NORDISK AS
摘要:The present invention provides novel compounds of Formula 1, compositions containing these compounds, 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, n wherein A, R 1 , R 2 , R 3 , R 4 , R 16 and R 17 are as defined in the specification. 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-9946236-A1
优先权日:1998-03-12
标题 :Modulators of protein tyrosine phosphatases (ptpases)
发明人：RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN
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 (PTPases) 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:EP-1062199-A1
优先权日:1998-03-12
标题 :Modulators of protein tyrosine phosphatases (ptpases)
发明人：RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOLLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN
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 (PTPases) 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:US-6051704-A
优先权日:1996-07-22
标题:Synthesis of macrocyclic tetraamido-N ligands
发明人：GORDON-WYLIE SCOTT W; COLLINS TERRENCE J
权利人:UNIV CARNEGIE MELLON
摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.

专利号:US-5783577-A
优先权日:1995-09-15
标题 :Synthesis of quinazolinone libraries and derivatives thereof
发明人：HOUGHTEN RICHARD A; OSTRESH JOHN M
权利人:TREGA BIOSCIENCES INC
摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.

专利号:WO-9710221-A1
优先权日:1995-09-15
标 题:Synthesis of quinazolinone libraries
发明人：HOUGHTEN RICHARD A; OSTRESH JOHN M
权利人:TORREY PINES INST
摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.