CAS: 42466-50-2; Thiophene-3-Carbaldehyde Oxime

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3-thiophene carboxaldehyde 3-formylthiophene diethyl acetal3-carbamoylthiophene (3-thienylmethyl)amine 4-methyl-N-(thiophen-3-ylmethyl)aniline

📜3-噻吩甲醛 在 盐酸羟胺,Sodium Carbonate体系中,用 乙醇,水作为反应溶剂,获得 Thiophene-3-Carbaldehyde Oxime
参考文献:烷基亚硝酸盐:新型试剂,可从醛糖肟和炔烃一次合成3,5-二取代的异恶唑
标题:烷基亚硝酸盐:新型试剂,可从醛糖肟和炔烃一次合成3,5-二取代的异恶唑
摘要:摘要 已经描述了一种有效的一锅法,该方法用于在常规加热条件下,使用亚硝酸烷基酯,由取代的醛肟(E和z的混合物)和炔烃合成3,5-二取代的异恶唑.合成异恶唑所需的关键腈氧化物中间体是通过用亚硝酸叔丁酯或亚硝酸异戊酯处理取代的醛肟而形成的.生成的腈氧化物在取代的炔烃上进行原位[3 + 2]偶极环加成反应,以高选择性或极高的产率选择性地生成3,5-二取代的异恶唑.已开发的合成方法用于合成先前报道的有效hdgat1抑制剂. 已经描述了一种有效的一锅法,该方法用于在常规加热条件下,使用亚硝酸烷基酯,由取代的醛肟(E和z的混合物)和炔烃合成3,5-二取代的异恶唑.合成异恶唑所需的关键腈氧化物中间体是通过用亚硝酸叔丁酯或亚硝酸异戊酯处理取代的醛肟而形成的.生成的腈氧化物在取代的炔烃上进行原位[3 + 2]偶极环加成反应,以高选择性或极高的产率选择性地生成3,5-二取代的异恶唑.已开发的合成方法用于合成先前报道的有效hdgat1抑制剂.
Doi:10.1055/S-0035-1561464

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-6166003-A
优先权日:1999-02-17
标 题 :Heterocyclic compounds for cancer chemoprevention
发明人：LAM LUKE K T
权利人:LKT LAB INC
摘要:A compound comprising a heterocyclic moiety, such as a thiophene, covalently attached to an alkylene isothiocyanate moiety. The compound is effective to prevent the occurrence or progression of cancer or a precancerous condition, and can be used for therapeutic or prophylactic purposes. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.