2,3-dichloro-5-(((tetrahydro-2H-pyran-2-yl)oxy)methyl)pyridine | 54127-61-6

• 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: 2,3-dichloro-5-(((tetrahydro-2H-pyran-2-yl)oxy)methyl)pyridine
• 英文别名: 2,3-dichloro-5-(oxan-2-yloxymethyl)pyridine
• CAS: 54127-61-6
• 化学式: C₁₁H₁₃Cl₂NO₂
• 分子量: 262.13
• InChiKey: MTLHVHGYDLIHHB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  31.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3,4-二氢-2H-吡喃 、 氯化亚锡二水合物 、 5,6-二氯-3-吡啶甲醇 在 silica gel 、 正己烷 、 乙酸乙酯 作用下， 以 氯仿 为溶剂， 反应 63.0h， 以The title compound (1.7 g) was obtained as colorless oil的产率得到2,3-dichloro-5-(((tetrahydro-2H-pyran-2-yl)oxy)methyl)pyridine
  参考文献：
  名称：

  Novel Heterocyclidene Acetamide Derivative

  摘要：

  一种由式（I′）表示的化合物：（其中m，n和p分别表示0至2；q表示0或1；R1表示卤素，烃基，杂环基，烷氧基，烷氧羰基基团，磺酰胺基，CN基团，NO2基团或类似基团；R2表示卤素，氨基，烃基，芳香杂环基或氧代基；X1表示O，—NR3—或—S（O）r-；X2表示亚甲基基团，O，—NR3—或—S（O）r-；Q'表示杂环芳基基团，杂环芳基烷基基团，取代芳基基团或芳基烷基基团；Cycle moiety表示芳环或杂环；波浪线表示E异构体或Z异构体），化合物的盐，或化合物或盐的溶剂化物。一种药物组合物和一种瞬时受体电位类型I（TRPV1）受体拮抗剂，均包含至少一种化合物，该化合物的盐或该化合物或盐的溶剂化物作为活性成分。

  公开号：

  US20080287428A1

文献信息

• Novel Heterocyclidene Acetamide Derivative
  申请人：Uchida Hideharu

  公开号：US20080287428A1

  公开（公告）日：2008-11-20

  A compound represented by formula (I′): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R 1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO 2 group, or the like; R 2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X 1 represents O, —NR 3 —, or —S(O)r-; X 2 represents a methylene group, O, —NR 3 —, or —S(O)r-; Q′ represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

  一个由式(I′)表示的化合物：（其中m、n和p分别表示0到2；q表示0或1；R1表示卤素、烃基、杂环基、烷氧基、烷氧羰基、磺酰胺基、CN基团、NO2基团等；R2表示卤素、氨基、烃基、芳香杂环基或醛基；X1表示O、—NR3—或—S(O)r-；X2表示亚甲基、O、—NR3—或—S(O)r-；Q′表示异芳基基团、异芳基烷基基团、取代芳基基团或芳基烷基基团；Cycle moiety代表芳基环或杂芳基环；波浪线表示E异构体或Z异构体），该化合物的盐，或该化合物或其盐的溶剂络合物。一种药物组合物和一种瞬时受体电位类型I（TRPV1）受体拮抗剂，每种包含至少一种该化合物、该化合物的盐，或该化合物或其盐的溶剂络合物作为活性成分。
• CONDENSED BENZAMIDE COMPOUNDS AND INHIBITORS OF VANILLOID RECEPTOR SUBTYPE 1 (VR1) ACTIVITY
  申请人：Koga Yoshihisa

  公开号：US20060035882A1

  公开（公告）日：2006-02-16

  To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt:

  提供一种对vanilloid受体亚型1（VR1）活性具有出色抑制作用的化合物，该化合物对于治疗与vanilloid受体亚型1（VR1）活性有关的疾病具有有效性，如疼痛、急性疼痛、慢性疼痛、神经病性疼痛、类风湿性关节炎疼痛、神经痛等，以及含有该化合物的药物组合物。该目标通过下面的式子所代表的缩合苯甲酰胺化合物（式子中的符号在说明书中定义了相同的含义）或其盐实现：
• FUSED BENZAMIDE COMPOUND AND VANILLOID RECEPTOR 1 (VR1) ACTIVITY INHIBITOR
  申请人：Japan Tobacco, Inc.

  公开号：EP1777225A1

  公开（公告）日：2007-04-25

  To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt:

  提供一种对香草素受体亚型 1（VR1）活性具有优异抑制作用的化合物，该化合物可有效治疗与香草素受体亚型 1（VR1）活性有关的疾病，如疼痛、急性疼痛、慢性疼痛、神经病理性疼痛、类风湿性关节炎疼痛、神经痛等，以及含有该化合物的药物组合物。由下式（式中符号与说明书中定义的含义相同）代表的缩合苯甲酰胺化合物或其盐已达到上述目的：
• NOVEL HETEROCYCLIDENE ACETAMIDE DERIVATIVE
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：EP1908753A1

  公开（公告）日：2008-04-09

  A compound represented by formula (I'): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, -NR3-, or -S(O)r-; X2 represents a methylene group, O, -NR3-, or - S(O)r-; Q' represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

  式 (I') 所代表的化合物： (其中 m、n 和 p 分别代表 0 至 2；q 代表 0 或 1；R1 代表卤素、烃基、杂环基、烷氧基、烷氧羰基、氨基磺酰基、CN 基、NO2 基或类似基团；R2 代表卤素、氨基、烃基、芳香杂环基或氧代基团；X1 代表 O、-NR3- 或 -S(O)r- ；X2代表亚甲基、O、-NR3-或-S(O)r-； Q'代表杂芳基、杂芳烷基、取代芳基或芳烷基；循环分子代表芳基环或杂芳环；波浪线代表E-异构体或Z-异构体）、化合物的盐、或化合物或盐的溶液。一种药物组合物和一种瞬时受体电位Ⅰ型（TRPV1）受体拮抗剂各自含有至少一种化合物、化合物的盐和化合物或盐的溶液作为活性成分。
• Condensed benzamide compounds as inhibitors of vanilloid receptor subtype 1 (VR1) activity
  申请人：Japan Tobacco, Inc.

  公开号：EP2314585A1

  公开（公告）日：2011-04-27

  To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt:

  提供一种对香草素受体亚型 1（VR1）活性具有优异抑制作用的化合物，该化合物可有效治疗与香草素受体亚型 1（VR1）活性有关的疾病，如疼痛、急性疼痛、慢性疼痛、神经病理性疼痛、类风湿性关节炎疼痛、神经痛等，以及含有该化合物的药物组合物。由下式（式中符号与说明书中定义的含义相同）代表的缩合苯甲酰胺化合物或其盐已达到上述目的：