2-氯-3-碘-4-甲基吡啶 | 926922-28-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 2-氯-3-碘-4-甲基吡啶
• 英文名称: 2-chloro-3-iodo-4-methylpyridine
• CAS: 926922-28-3
• 化学式: C₆H₅ClIN
• 分子量: 253.47
• InChiKey: ZWXCPWVRUTYWCA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  1

安全信息

• 危险等级：
  IRRITANT
• 海关编码：
  2933399090
• 危险性防范说明：
  P280,P305+P351+P338,P310
• 危险性描述：
  H302,H315,H319,H332,H335

反应信息

• 作为反应物：
  描述：

  2-氯-3-碘-4-甲基吡啶 在 吡啶 、 一水合肼 、 三氯氧磷 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 生成
  参考文献：
  名称：

  Indolin-2-one p38α inhibitors III: Bioisosteric amide replacement

  摘要：

  Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38 alpha inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.09.006
• 作为产物：
  描述：

  2-氯-3-氨基-4-甲基吡啶 在 盐酸 、 sodium nitrite 、 potassium iodide 作用下， 以 水 为溶剂， 以58%的产率得到2-氯-3-碘-4-甲基吡啶
  参考文献：
  名称：

  New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors

  摘要：

  这项发明涉及具有一般式(I)的新p38丝裂原活化蛋白激酶抑制剂；其制备方法；包含它们的药物组合物；以及它们在治疗中的应用。

  公开号：

  EP2113503A1

文献信息

• RADIOLABELLED mGluR2 PET LIGANDS
  申请人：Andrés-Gil José Ignacio

  公开号：US20130230459A1

  公开（公告）日：2013-09-05

  The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.

  本发明涉及新型的、选择性的、放射性标记的mGluR2配体，这些配体可用于使用正电子发射断层扫描（PET）在组织中成像和量化代谢型谷氨酸受体mGluR2。本发明还涉及包含这些化合物的组合物，制备这些化合物和组合物的方法，使用这些化合物和组合物在体外或体内成像组织、细胞或宿主，以及所述化合物的前体。
• [EN] HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS<br/>[FR] COMPOSÉS HÉTÉRO-AROMATIQUES ET LEUR UTILISATION EN TANT QUE LIGANDS D1 DE LA DOPAMINE
  申请人：PFIZER

  公开号：WO2014207601A1

  公开（公告）日：2014-12-31

  The present invention provides, in part, compounds of Formula (I) and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1 -mediated (or D1 -associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.

  本发明部分提供了Formula (I)的化合物及其药用盐；其制备方法；制备中使用的中间体；含有这种化合物或盐的组合物，以及它们用于治疗D1介导的（或与D1相关的）疾病，包括但不限于精神分裂症（例如，其认知和消极症状）、认知障碍（例如，与精神分裂症、阿尔茨海默病、帕金森病或药物治疗相关的认知障碍）、年龄相关的认知衰退、痴呆症和帕金森病。
• [EN] HERBICIDAL PYRIDAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS HERBICIDES DE PYRIDAZINONE
  申请人：SYNGENTA LTD

  公开号：WO2013050421A1

  公开（公告）日：2013-04-11

  The present invention provides a compound of Formula (I) or an agronomically acceptable salt thereof, wherein:R2 is selected from the group consisting of (A1), (A2) and (A3) wherein X1 is N or CR7 X2 is N or CR8 X3 is N or CR9 X4 is N or CR6 R1, R3, R4, R5 R6, R7, R8 and R9 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.

  本发明提供了一种式（I）的化合物或其农业上可接受的盐，其中：R2选自由（A1）、（A2）和（A3）组成的群，其中X1为N或CR7，X2为N或CR8，X3为N或CR9，X4为N或CR6，R1、R3、R4、R5、R6、R7、R8和R9如本文所定义。该发明还涉及包括式（I）的化合物的除草剂组合物，以及它们在控制杂草方面的用途，特别是在有用植物作物中。
• New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
  申请人：Laboratorios Almirall, S.A.

  公开号：EP2113503A1

  公开（公告）日：2009-11-04

  This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.

  这项发明涉及具有一般式(I)的新p38丝裂原活化蛋白激酶抑制剂；其制备方法；包含它们的药物组合物；以及它们在治疗中的应用。
• ISOQUINOLINES AS INHIBITORS OF HPK1
  申请人：Genentech, Inc.

  公开号：US20180282282A1

  公开（公告）日：2018-10-04

  Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.

  描述了异喹啉化合物及其作为HPK1（造血激酶1）抑制剂的用途。这些化合物在治疗依赖于HPK1的疾病和增强免疫应答方面非常有用。还描述了抑制HPK1的方法、治疗依赖于HPK1的疾病的方法、增强免疫应答的方法，以及制备异喹啉化合物的方法。