Picolinsaeurechlorid

• 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
• 英文名称: Picolinsaeurechlorid
• 英文别名: Chloro pyridine-2-carboxylate
• 化学式: C₆H₄ClNO₂
• 分子量: 157.556
• InChiKey: JZUQLLLMKCOKSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  39.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Picolinsaeurechlorid 、 二环己胺 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 N,N-dicyclohexyl-pyridineamide
  参考文献：
  名称：

  Efficient Synthesis of Isoquinolines via Rh(III)-Catalyzed Oxidative Annu­lation of Picolinamides with Alkynes

  摘要：

  An efficient synthesis of isoquinolines via Rh(III)-catalyzed oxidative annulation of picolinamides with alkynes using Cu(OAc)(2) as an oxidant has been developed. The scope of the reaction was studied with a selection of various picolinamides and alkynes, and the desired isoquinolines were obtained in good to excellent yields.

  DOI：

  10.1055/s-0033-1340870
• 作为产物：
  描述：

  2-吡啶甲酸 在 氯化亚砜 、 N,N-二甲基甲酰胺 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 生成 Picolinsaeurechlorid
  参考文献：
  名称：

  Efficient Synthesis of Isoquinolines via Rh(III)-Catalyzed Oxidative Annu­lation of Picolinamides with Alkynes

  摘要：

  An efficient synthesis of isoquinolines via Rh(III)-catalyzed oxidative annulation of picolinamides with alkynes using Cu(OAc)(2) as an oxidant has been developed. The scope of the reaction was studied with a selection of various picolinamides and alkynes, and the desired isoquinolines were obtained in good to excellent yields.

  DOI：

  10.1055/s-0033-1340870

文献信息

• [EN] DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS<br/>[FR] PHARMACOPHORES DUALS, ANTAGONISTES DES RÉCEPTEURS MUSCARINIQUES ET INHIBITEURS DE L'ACTIVITÉ PDE4
  申请人：GLAXO GROUP LTD

  公开号：WO2009100169A1

  公开（公告）日：2009-08-13

  The present invention is directed to novel compounds of Formula's (I) - (VI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of and/or prophylaxis of respiratory diseases, including inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

  本发明涉及式(I) - (VI)的新化合物，以及其药学上可接受的盐、药物组合物及其在治疗中的应用，例如作为磷酸二酯酶IV (PDE4)的抑制剂和肌碱乙酰胆碱受体 (mAChRs)的拮抗剂，用于治疗和/或预防呼吸道疾病，包括炎症性和/或过敏性疾病，如慢性阻塞性肺病（COPD）、哮喘、鼻炎（例如过敏性鼻炎）、特应性皮炎或银屑病。
• 6-AMINO-2-SUBSTITUTED-5-VINYLSILYLPYRIMIDINE-4-CARBOXYLIC ACIDS AND ESTERS AND 4-AMINO-6-SUBSTITUTED-3-VINYLSILYLPYRIDINE-2-CARBOXYLIC ACIDS AND ESTERS AS HERBICIDES
  申请人：Eckelbarger Joseph D.

  公开号：US20120190549A1

  公开（公告）日：2012-07-26

  6-Amino-2-substituted-5-vinylsilylpyrimidine-4-carboxylates and 4-amino-6-substituted-3-vinylsilylpyridine-picolinates and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control

  6-氨基-2-取代-5-乙烯基硅基嘧啶-4-羧酸酯和4-氨基-6-取代-3-乙烯基硅基吡啶-哌啶酸酯及其胺和酸衍生物是有效的除草剂，展示了广泛的杂草控制谱。
• [EN] SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS DE PYRAZOLO[1,5-A]PYRIDINE SUBSTITUÉS EN TANT QU'INHIBITEURS DE LA KINASE RET
  申请人：ANDREWS STEVEN W

  公开号：WO2018071454A1

  公开（公告）日：2018-04-19

  Provided herein are compounds of the Formula I: (I) or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

  本文提供了Formula I的化合物：(I)或其药用可接受的盐或溶剂，其中A、B、X1、X2、X3、X4、环D、E、Ra、Rb、n和m的含义如规范中所述，它们是RET激酶的抑制剂，并且在治疗和预防可以用RET激酶抑制剂治疗的疾病中非常有用，包括与RET相关的疾病和紊乱。
• [EN] DIHYDROPYRIMIDINONES FOR USE AS BACE2 INHIBITORS<br/>[FR] DIHYDROPYRIMIDINONES POUR UTILISATION EN TANT QU'INHIBITEURS DE BACE2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2010128058A1

  公开（公告）日：2010-11-11

  This invention relates to dihydropyrimidinones of the formula (I), wherein X and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.

  这项发明涉及公式（I）中的二氢嘧啶酮，其中X和R1至R7如描述和索赔中定义的那样，以及其药学上可接受的盐。这些化合物是BACE2抑制剂，可用作治疗或预防疾病如糖尿病的药物。
• 6-(Poly-substituted aryl)-4-aminopicolinates and their use as herbicides
  申请人：Balko W. Terry

  公开号：US20070179060A1

  公开（公告）日：2007-08-02

  4-Aminopicolinic acids having tri- and tetra-substituted aryl substituents in the 6-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.

  在6位具有三取代和四取代芳基取代基的4-氨基吡啶酸及其胺和酸衍生物是一类高效除草剂，展示出广泛的杂草控制谱。