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7-氯-6-氮杂吲哚置于sodium Tetrahydroborate,1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,四甲基乙二胺体系中,用 四氢呋喃 用作溶剂,化学反应 60.0H,以70.95%的收率获得6-氮杂吲哚
参考文献:新型吲哚和氮杂吲哚(吡咯并吡啶)大麻素(cb)受体激动剂:设计,合成,结构-活性关系,理化性质和生物活性
标题:新型吲哚和氮杂吲哚(吡咯并吡啶)大麻素(cb)受体激动剂:设计,合成,结构-活性关系,理化性质和生物活性
摘要:报告了一系列新型的大麻素1(cb 1)和大麻素2(cb 2)受体配体的发现,合成和构效关系(sar).基于所述aminoalkylindole类大麻素受体激动剂,联苯部分被引入作为新颖的亲脂性的吲哚3-酰基取代基在11-16.此外,系绳是与羧酰胺接头取代-3-羰基17-20和氮杂吲哚(吡咯并吡啶)核被设计为具有改进的物理化学性质的吲哚生物电子等排在21-25.通过这些sar努力,几个高亲和力cb 1 / Cb 2确定了双重大麻素受体配体.吲哚-3-羧酰胺17对cb 1比cb 2受体具有几位数的纳摩尔亲和力和约80倍的选择性.氮杂吲哚显示出显着改善的理化性质(亲脂性;水溶性).氮杂吲哚21引起有效的大麻素活性.大麻素受体激动剂17和21在大麻素受体调节的神经传递的急性大鼠脑切片模型中有效地调节了兴奋性突触传递.
Doi:10.1016/j.Ejmech.2011.08.021

专利信息

专利号:US-7425629-B2
优先权日:2005-09-30
标 题:Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
发明人：SONG JINHUA J; REEVES JONATHAN T; ROSCHANGAR FRANK; TAN ZHULIN; YEE NATHAN K
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:A process for stereoselective synthesis of a compound of Formula (I) n nwherein R 1 , R 2 , R 3 , R 4 , and R 5 are as described herein.

专利号:WO-9946268-A1
优先权日:1998-03-12
标题 :MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPases)
发明人：ANDERSEN HENRIK SUNE; JONES TODD KEVIN; HOLSWORTH DANIEL DALE
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-2002019412-A1
优先权日:1998-03-12
标题:Modulators of protein tyrosine phosphatases (ptpases)
发明人：ANDERSEN HENRIK SUNE; JONES TODD KEVIN; HOLSWORTH DANIEL DALE
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.

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-11485721-B2
优先权日:2017-11-21
标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses
发明人：KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN
权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST
摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

专利号:WO-2008103866-A1
优先权日:2007-02-22
标题 :Synthesis of indoles
发明人：TALLEY JOHN JEFFREY; RENZE JUERGEN T
权利人:MICROBIA INC; TALLEY JOHN JEFFREY; RENZE JUERGEN T
摘要:Method for preparing indoles, including methods that permit high yield production of particular compounds, are described.