1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine | 43213-61-2

• 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: 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine
• 英文别名: 1,2,3,4-tetrahydro-benzo[4,5]furo[3,2-c]pyridine；benzofuro[3,2-c]-1,2,3,4-tetrahydropyridine；Benzofuro[3,2-c]pyridine, 1,2,3,4-tetrahydro-；1,2,3,4-tetrahydro-[1]benzofuro[3,2-c]pyridine
• CAS: 43213-61-2
• 化学式: C₁₁H₁₁NO
• 分子量: 173.214
• InChiKey: OGOWMVYFFWEWQT-UHFFFAOYSA-N

物化性质

• 沸点：
  302.7±32.0 °C(Predicted)
• 密度：
  1.160±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  25.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine 在 platinum(IV) oxide 氢气 作用下， 以 三氟乙酸 为溶剂， 生成 (4ar,9bc)-1,2,3,4,4a,9b-hexahydro-benzo[4,5]furo[3,2-c]pyridine
  参考文献：
  名称：

  Reduction of 1,2,3,4-tetrahydro- to 1,2,3, 4,4a,9b-hexahydrobenzofuro[3,2-c]pyridines

  摘要：

  DOI：

  10.1007/bf00473833
• 作为产物：
  描述：

  苯并呋喃-2-羧酸 在 喹啉 、 盐酸 、 正丁基锂 、 铜 、 三乙胺 、 sodium iodide 作用下， 以 乙醚 、 乙醇 、 氯仿 、 丙酮 为溶剂， 生成 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine
  参考文献：
  名称：

  New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2- c ]pyridine having highly active and potent central α 2 -antagonistic activity as potential antidepressants

  摘要：

  The synthesis and biological activity of a series of benzofuro[3,2-c]pyridines and a benzothieno[3,2-c]pyridine are described. These compounds exhibit high affinity for the alpha(2)-adrenoceptor, with high selectivity versus the alpha(1)-receptor. Compound 1 also shows potent in vivo central activity and has been selected for further biological and clinical evaluation. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00591-0

文献信息

• Npy antagonists, preparation and uses
  申请人：Botez Iuliana

  公开号：US20090233910A1

  公开（公告）日：2009-09-17

  The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.

  本发明涉及新颖化合物，它们的制备和用途，特别是在治疗方面的用途。更具体地说，它涉及至少具有两个芳香环的衍生化合物，它们的制备和用途，特别是在人类或动物健康领域。这些化合物对存在于中枢和外周神经系统中的神经肽Y（NPY）的生物受体具有亲和力。本发明的化合物优选为NPY拮抗剂，更具体地说是NPY Y1亚型的拮抗剂，因此可用于治疗或预防涉及NPY的任何疾病。本发明还涉及含有所述化合物的药物组合物，其制备和用途，以及使用所述化合物的治疗方法。
• Novel Compound - 827
  申请人：Dossetter Alexander Graham

  公开号：US20090012077A1

  公开（公告）日：2009-01-08

  The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.

  本发明涉及用于治疗与半胱氨酸蛋白酶活性相关疾病的化合物和组合物。这些化合物是半胱氨酸蛋白酶的可逆抑制剂，包括卡特普辛B、K、C、F、H、L、O、S、W和X。特别感兴趣的是与卡特普辛K相关的疾病。
• Tricylic delta 3-piperidines as pharmaceuticals
  申请人：Janssen Pharmaceutica N.V.

  公开号：US06352999B1

  公开（公告）日：2002-03-05

  The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; n is 1 or 2; X is —O—, —S—, —S(═O)— or —S(═O)2—; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is an indole, a benzisoxazole, a benzisothiazole, a 2H-benzopyranone, a phenoxyphenyl, a benzamide, a benzophenone or a benzopyrimidinone having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

  本发明涉及公式N-氧化物形式的化合物，其药学上可接受的加盐物和立体化学异构形式，其中Alk为C1-6烷二基；n为1或2；X为—O—、—S—、—S(═O)—或—S(═O)2—；每个R1独立地为氢、卤素、C1-6烷基、硝基、羟基或C1-4烷氧基；D为吲哚、苯并异噁唑、苯并噻唑、2H-苯并吡喃酮、苯氧苯基、苯甲酰胺、苯甲酮或具有中枢α2-肾上腺素受体拮抗活性的苯基吡啶酮。它还涉及它们的制备、药用和组合物。
• Preparation and pharmacological examination of a number of derivatives of tetrahydrobenzofuropyridine
  作者：L. A. Aksanova、N. K. Barkov、V. A. Zagorevskii、N. F. Kucherova、L. M. Sharkova

  DOI：10.1007/bf01145653

  日期：1975.1

  3-chloropropionyl chloride to give the corresponding chloropropionyl derivatives (III) and (IV), respectively. Analogously, (II) and 4-chlorobutyry! chloride gave the compound (V). These N-~-chloroacyl derivatives of the starting materials gave on reaction with secondary bases a series of corresponding amino derivatives (VI), (VII), (VIII), and (IX). Alkylation of (II) with 2-dimethylaminoethyl, 3-dimethylaminopropyl

  1,2,3,4-四氢苯并呋喃E3,2-~]吡啶(1)及其4-甲基同系物(II)，均由我们之前描述过[5]，在氮原子上用3-氯丙酰氯酰化得到分别为相应的氯丙酰基衍生物 (III) 和 (IV)。类似地，(II) 和 4-氯丁酸！氯化得到化合物(V)。原料的这些N--氯酰基衍生物与仲碱反应得到一系列相应的氨基衍生物(VI)、(VII)、(VIII)和(IX)。(II)与2-二甲氨基乙基、3-二甲氨基丙基和3-N'-甲基哌嗪丙基氯化物的烷基化分别得到二胺(X)和(XI)以及三胺(XII)。化合物(XIII)和(XIV)分别由(I)和(II)通过用3-对-氟苯甲酰丙基氯处理(见表i)获得。
• INHIBITORS OF NUCLEOPHOSMIN (NPM) AND METHODS FOR INDUCING APOPTOSIS
  申请人：Mahadevan Daruka

  公开号：US20080221146A1

  公开（公告）日：2008-09-11

  Nucleophosmin inhibitors are disclosed which inhibit the multimerization of nucleophosmin and the biological activity of nucleophosmin, such as the ability of nucleophosmin to inhibit apoptosis and inhibit cellular differentiation. These small molecule inhibitors are useful for treating diseases and disorders, such as cancer associated with dysregulated nucleophosmin expression. Methods for identifying small molecule inhibitors of nucleophosmin involving multimerization sites for nucleophosmin are also disclosed. An exemplary small molecule inhibitor of nucleophosmin is NSC348884 which has the following chemical structure:

  揭示了抑制核磷蛋白多聚化和核磷蛋白生物活性的核磷蛋白抑制剂，例如核磷蛋白抑制凋亡和抑制细胞分化的能力。这些小分子抑制剂可用于治疗与核磷蛋白表达失调相关的癌症等疾病和疾病。还披露了识别核磷蛋白小分子抑制剂的方法，涉及核磷蛋白的多聚化位点。核磷蛋白的一个示例小分子抑制剂是NSC348884，其化学结构如下：