(5-iodo-benzofuran-2-yl)-methanol | 690265-42-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: (5-iodo-benzofuran-2-yl)-methanol
• 英文别名: (5-iodo-1-benzofuran-2-yl)methanol
• CAS: 690265-42-0
• 化学式: C₉H₇IO₂
• 分子量: 274.058
• InChiKey: OMSMQBSLRVTLOF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  33.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (5-iodo-benzofuran-2-yl)-methanol 在 三溴化磷 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 2-bromomethyl-5-iodo-benzofuran
  参考文献：
  名称：

  Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation

  摘要：

  The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for A beta fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for A beta fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC(50) = 0.07 and 0.08 mu M, respectively) than those of Curcumin (IC(50) = 0.80 mu M) and IMSB (IC(50) = 8.00 mu M) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.08.111
• 作为产物：
  描述：

  5-碘水杨醛 在 lithium aluminium tetrahydride 、 potassium carbonate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 4.33h， 生成 (5-iodo-benzofuran-2-yl)-methanol
  参考文献：
  名称：

  2’-羰基-3-溴-螺[苯并呋喃-2,4’-噁唑烷酮] 类化合物及其制备方法

  摘要：

  本发明公开了一种2’‑羰基‑3‑溴‑螺[苯并呋喃‑2,4’‑噁唑烷酮]类化合物及其制备方法。2’‑羰基‑3‑溴‑螺[苯并呋喃‑2,4’‑噁唑烷酮]类化合物为结构式如式Ⅱ所示的光活性的化合物。本发明提供的2’‑羰基‑3‑溴‑螺[苯并呋喃‑2,4’‑噁唑烷酮]类化合物，是一种具有光学活性的螺环化合物，它可以利用不同的反应条件进行3‑位溴原子的取代反应，得到多种官能团取代的具有光学活性的手性螺环化合物，如叠氮基、羟基、烯丙基和苯甲醚基取代的光活性手性螺环化合物。因此本发明提供了一种能够利用该溴原子发生取代反应，从而制备多种不同种类的具有光活性的其它手性螺环化合物，丰富和补充了此类型化合物的范围，具有很大的潜在应用价值。

  公开号：

  CN106588952B

文献信息

• Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：US20040209865A1

  公开（公告）日：2004-10-21

  The present invention relates to alkyne compounds of general formula I 1 wherein the groups and residues A, B, W, X, Y, Z, R 1 and R 2 have the meanings given in claim 1 . The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的炔烃化合物 1 其中基团和残基A、B、W、X、Y、Z、R 1 和R 2 具有权利要求中给出的含义。本发明还涉及含有根据本发明至少一种炔烃的药物组合物。鉴于它们的MCH受体拮抗活性，根据本发明的药物组合物适用于治疗代谢紊乱和/或进食紊乱，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。
• Bicyclic aromatic substituted pyridone derivative
  申请人：Sakuraba Shunji

  公开号：US20090264426A1

  公开（公告）日：2009-10-22

  Disclosed is a compound represented by the formula (I): Wherein R 1 and R 2 independently represent a hydrogen atom, a lower alkyl group or the like; X 1 , X 2 and X 3 independently represent a methine group or a nitrogen atom; Y 1 and Y 3 independently represent a single bond, —O— or the like; Y 2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z 1 and Z 2 independently represent a single bond, a C 1-4 alkylene group or the like; Ar 1 represents an aromatic carbocyclic ring or the like; and Ar 2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

  本发明揭示了一种化合物，其化学式为（I）：其中R1和R2分别代表氢原子、低碳烷基或类似物；X1、X2和X3分别代表亚甲基基团或氮原子；Y1和Y3分别代表单键、—O—或类似物；Y2代表低碳烷基基团或类似物；W1至W4独立地代表单键、亚甲基基团或类似物；L代表单键、亚甲基基团或类似物；Z1和Z2独立地代表单键、C1-4烷基基团或类似物；Ar1代表芳香环烷基环或类似物；Ar2代表双环芳香环烷基环或类似物。该化合物可用作治疗中枢疾病、心血管疾病或代谢性疾病的药物。
• ALKYNE COMPOUNDS WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
  申请人：Stenkamp Dirk

  公开号：US20090069282A1

  公开（公告）日：2009-03-12

  The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R 1 and R 2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的炔化合物，其中A、B、W、X、Y、Z、R1和R2的基团和残基具有权利要求1中给出的含义。本发明还涉及包含至少一种根据本发明的炔烃的制药组合物。鉴于它们的MCH受体拮抗活性，根据本发明的制药组合物适用于治疗代谢性疾病和/或进食障碍，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。
• Chiral Phosphine Oxide–Sc(OTf)₃ Complex Catalyzed Enantioselective Bromoaminocyclization of 2-Benzofuranylmethyl <i>N</i>-Tosylcarbamates. Approach to a Novel Class of Optically Active Spiro Compounds
  作者：Zequan Li、Yian Shi

  DOI：10.1021/acs.orglett.5b02817

  日期：2015.12.4

  An efficient enantioselective bromoaminocyclization of 2-benzofuranylmethyl N-tosylcarbamates catalyzed by a chiral phosphine oxide-Sc(OTf)(3) complex is described. A wide variety of optically active spiro benzofuran oxazolidinones can be obtained with high enantioselectivities.
• NEUE ALKIN-VERBINDUNGEN MIT MCH-ANTAGONISTISCHER WIRKUNG UND DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：EP1558578B1

  公开（公告）日：2013-03-13