CAS: 98437-23-1; Benzo[b]Thiophen-2-Ylboronic Acid

该化合物是一种热循环碳酸衍生物,广泛用于铃木-米亚乌拉交叉相交反应,这是形成有机合成中碳-碳联系的关键方法.本祖[b]thiophene核心提供了一个硬性,芳香框架,加强了催化变的稳定性和反应性.本氏酸功能组能够与丙烯或乙烯卤化物有效结合,使其对在制药,农用化学和材料科学中制造复杂分子很有价值.化合物在普通有机溶剂中表现出良好的溶性,便于合成应用的处理.其持续性能和与多种反应条件的兼容性使得它成为先进的有机合成的可靠试剂.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

  • 合成目标产物 Benzo[b]Thien-2-Ylboronic Acid 主要起始原料 Trimethyl Borate And Thianaphthene
  • (文献来源)合成步骤主要原料 Trimethyl Borate 和 Thianaphthene
苯并噻吩置于叔丁基锂体系中,用78%的收率获得产物苯并噻吩-2-硼酸
参考文献:N-Aryl Thienyl-,Furyl-,And Pyrrolyl-Sulfonamides And Derivatives Thereof That Modulate The Activity Of Endothelin
标题:N-Aryl Thienyl-,Furyl-,And Pyrrolyl-Sulfonamides And Derivatives Thereof That Modulate The Activity Of Endothelin
摘要:提供了噻吩基,呋喃基和吡咯基磺酰胺以及用于调节或改变内皮素肽家族活性的方法.特别是,提供了n-(异恶唑基)噻吩磺酰胺,N-(异恶唑基)呋喃磺酰胺和n-(异恶唑基)吡咯磺酰胺以及使用这些磺酰胺通过将受体与磺酰胺接触来抑制内皮素肽与内皮素受体结合的方法.还提供了通过施用有效量的一个或多个这些磺酰胺或其前药来治疗内皮素介导的疾病的方法,这些磺酰胺或其前药抑制或增加内皮素的活性.

海关参考信息

专利信息


专利号:WO-2011106986-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO
权利人:MERCK SHARP & DOHME; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO
摘要:Compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and /or viral production in a cell-based system. Wherein Z, R 30 , R 40 , R 50 and R 60 of compounds of formula (I) are herein defined as in the description.

专利号:US-2012328569-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
权利人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
摘要:Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase 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-9549917-B2
优先权日:2011-09-08
标 题 :Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS
权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase 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-8207337-B2
优先权日:2007-01-29
标 题:Reagent for organic synthesis reaction containing organic triol borate salt
发明人:MIYAURA NORIO; YAMAMOTO YASUNORI
权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD
摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).

专利号:RU-2147582-C1
优先权日:1995-03-31
标 题:Method of synthesis of 2-substituted benzo[b]thiophene (variants), method of synthesis of derivatives of 2-phenyl-3-aroylbenzo[b]thiophene (variants) and derivatives of benzo[b]thiophene

专利号:US-2009030208-A1
优先权日:2005-04-08
标题 :(+) - and (-) -8-Alkyl-3-(Trifluoralkylsulfonyloxy)-8-Azabicyclo(3.2.1.)Oct-2-Ene
发明人:PETERS DAN; OLESEN DORTHE FILTENBORG; DAM EVA
权利人:PETERS DAN; OLESEN DORTHE FILTENBORG; DAM EVA
摘要:This invention relates to novel enantiopure compounds, useful as starting material for synthesis of enantiopure pharmaceuticals. n In other aspects the invention relates to a method of preparing the enantiopure compounds of the invention.
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主要参考文献

[参考文献]: Anna Minkkil, Et Al. Discovery Of Boronic Acids As Novel And Potent Inhibitors Of Fatty Acid Amide Hydrolase. J Med Chem. 2008 Nov 27;51(22):7057-60.
[参考文献]: Steven R Inglis, Et Al. Synthesis And Evaluation Of 3-(Dihydroxyboryl)Benzoic Acids As D,D-Carboxypeptidase R39 Inhibitors. J Med Chem. 2009 Oct 8;52(19):6097-106.

合成参考文献


摘要:Aitken, R. A.; Meehan, A., Science of Synthesis Knowledge Updates, (2014) 3, 159.
摘要:Aitken, R. A.; Meehan, A., Science of Synthesis Knowledge Updates, (2014) 3, 195.
摘要:MacMillan, D. W. C.; Watson, A. J. B., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 363.
摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 253.
摘要:Carboni, B.; Berrée, F., Science of Synthesis: Multicomponent Reactions, (2013) 1, 225.
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