7-bromo-1-methyl-3,4-dihydroisoquinoline | 371221-50-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氢异喹啉
• 英文名称: 7-bromo-1-methyl-3,4-dihydroisoquinoline
• CAS: 371221-50-0
• 化学式: C₁₀H₁₀BrN
• 分子量: 224.1
• InChiKey: WKXOECKPJPOIBK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  12.4
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  7-bromo-1-methyl-3,4-dihydroisoquinoline 在 ammonium hydroxide 、 hydroxylamine-O-sulfonic acid 作用下， 以 甲醇 为溶剂， 反应 48.0h， 以71%的产率得到1-methyl-8-bromo-1,2,3,7b-tetrahydro-1,1a-diazacyclopropa[α]naphthalene
  参考文献：
  名称：

  Synthesis and characterization of a diaziridinium ion. Conversion of 3,4-dihydroisoquinolines to 4,5-dihydro-3H-benzo[2,3]diazepines via a formal N-insertion process

  摘要：

  DOI：

  10.1016/j.tet.2014.03.015
• 作为产物：
  描述：

  4-溴苯乙胺 在 草酰氯 、 三氯化铁 、 三乙胺 作用下， 以 氯仿 为溶剂， 生成 7-bromo-1-methyl-3,4-dihydroisoquinoline
  参考文献：
  名称：

  Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties

  摘要：

  A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.10.026

文献信息

• [EN] TETRAHYDROISOQUINOLINE DERIVATIVES<br/>[FR] DÉRIVÉS DE TÉTRAHYDROISOQUINOLINE
  申请人：UCB BIOPHARMA SPRL

  公开号：WO2016055479A1

  公开（公告）日：2016-04-14

  The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.

  本发明涉及公式（I）所示的四氢异喹啉衍生物，它们是D1的正向变构调节剂，因此在D1受体发挥作用的疾病治疗中作为药物剂有益。
• [EN] PLASMA KALLIKREIN INHIBITORS<br/>[FR] INHIBITEURS DE LA KALLICRÉINE PLASMATIQUE
  申请人：KALVISTA PHARMACEUTICALS LTD

  公开号：WO2021028645A1

  公开（公告）日：2021-02-18

  The present invention provides compounds of formula (I): (I) compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, A, B, W, X, Y and Z are as defined herein.

  本发明提供式(I)化合物：(I)包含此类化合物的组合物；此类化合物在治疗中的应用（例如在治疗或预防与血浆激肽释放酶活性相关的疾病或状况中的应用）；以及使用此类化合物治疗患者的方法；其中R5、R6、R7、A、B、W、X、Y和Z如本文所定义。
• A highly efficient asymmetric synthesis of quaternary stereocenter-containing indolizidine and quinolizidine alkaloids using aldehydes, nitroalkenes, and unactivated cyclic ketimines
  作者：Yu Tan、Yong-Jian Chen、Hua Lin、Han-Lin Luan、Xing-Wen Sun、Xiao-Di Yang、Guo-Qiang Lin

  DOI：10.1039/c4cc07703b

  日期：——

  A highly efficient approach for the construction of indolizidines and quinolizidines bearing a bridged quaternary stereocenter has been established in a one-pot fashion using aldehydes, nitroalkenes, and cyclic ketimines with excellent enantioselectivities and in high yields. Moreover, this method could be applied to the synthesis of indolizidines in the gram scale.

  已经建立了一种高效的构建带有桥联四级立体中心的吲哚并立核苷和喹喔啉类的方法，该方法使用具有优异对映选择性和高收率的醛，硝基烯和环状酮亚胺以一锅法建立。而且，该方法可以用于克级的吲哚并立定的合成。
• Iron-Catalyzed Stereoselective Allylboration of 3,4-Dihydroisoquinolines with Potassium Allyltrifluoroborates
  作者：Yong Fang、Xiaoling Hu、Yunfei Luo、Zhuangzhuang Shi、Xu Zhao、Raveendra Reddy Gopireddy

  DOI：10.1055/a-1493-6420

  日期：2021.10

  An iron-catalyzed allyation of isoquinoline with potassium allyltrifluoroborate is described. The operation of this reaction is very simple and highly practical. The diastereoisomer having two adjacent chiral centers were obtained in single anti-configuration.

  描述了异氟喹啉与烯丙基三氟硼酸钾的铁催化的烯丙基化。该反应的操作非常简单并且非常实用。具有两个相邻手性中心的非对映异构体以单一抗构型获得。
• [EN] NAPHTHAMIDINE UROKINASE INHIBITORS<br/>[FR] INHIBITEUR DE NAPHTHAMIDINE UROKINASE
  申请人：ABBOTT LAB

  公开号：WO2001081314A1

  公开（公告）日：2001-11-01

  Compounds having formula (I) are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.

  式(I)的化合物是尿激酶抑制剂，并可用于治疗与尿激酶有关的疾病。还公开了抑制尿激酶的组合物、制备尿激酶抑制剂的方法以及抑制哺乳动物体内尿激酶的方法。