4-methyl-N-(5-nitropyridin-2-yl)benzenesulfonamide | 65523-68-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-methyl-N-(5-nitropyridin-2-yl)benzenesulfonamide
• 英文别名: 4-methyl-N-(5-nitro-2-pyridinyl)benzenesulfonamide
• CAS: 65523-68-4
• 化学式: C₁₂H₁₁N₃O₄S
• mdl: MFCD03381356
• 分子量: 293.303
• InChiKey: NRJYXDGOFKYSCZ-UHFFFAOYSA-N

物化性质

• 沸点：
  485.6±55.0 °C(Predicted)
• 密度：
  1.467±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  113
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-methyl-N-(5-nitropyridin-2-yl)benzenesulfonamide 在 palladium 10% on activated carbon 氢气 、 甲酸铵 作用下， 以 甲醇 、 水 为溶剂， 反应 4.0h， 以42%的产率得到N-(5-aminopyridin-2-yl)-4-methylbenzenesulfonamide
  参考文献：
  名称：

  AROMATIC SULFONE COMPOUND AS ALDOSTERONE RECEPTOR MODULATOR

  摘要：

  本发明提供了以下式（I）所表示的化合物： [其中，A表示以下式（A-1）的基团： 等等，R1和R2分别独立表示氢原子等，Z表示CR3等，W表示CR4等，Q表示CR5等，R3、R4和R5分别独立表示氢原子等，Y表示氧原子或硫原子，X表示氧原子等，B表示可选择地取代的芳基或可选择地取代的杂环基]，其前药或其药学上可接受的盐，用于预防或治疗高血压、脑卒中、心力衰竭等各种疾病。

  公开号：

  EP1844768A1
• 作为产物：
  描述：

  2-溴-5-硝基吡啶 、 对甲苯磺酰胺 在 copper(l) iodide 、 potassium carbonate 、 (1S,2S)-(+)-N,N'-二甲基环己烷-1,2-二胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以72%的产率得到4-methyl-N-(5-nitropyridin-2-yl)benzenesulfonamide
  参考文献：
  名称：

  Copper-Mediated N-Heteroarylation of Primary Sulfonamides: Synthesis of Mono-N-heteroaryl Sulfonamides

  摘要：

  We describe the coupling of primary sulfonamides and various halogenated heterocyclic cores, with an emphasis on 2-heteroaryl halides, via copper catalysis. These studies enabled the synthesis of many new mono-N-heteroaryl sulfonamides. The electronic factors that influence the course of the reaction have also been Investigated.

  DOI：

  10.1021/ol100263r

文献信息

• Bicyclic aromatic substituted pyridone derivative
  申请人：Sakuraba Shunji

  公开号：US20090264426A1

  公开（公告）日：2009-10-22

  Disclosed is a compound represented by the formula (I): Wherein R 1 and R 2 independently represent a hydrogen atom, a lower alkyl group or the like; X 1 , X 2 and X 3 independently represent a methine group or a nitrogen atom; Y 1 and Y 3 independently represent a single bond, —O— or the like; Y 2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z 1 and Z 2 independently represent a single bond, a C 1-4 alkylene group or the like; Ar 1 represents an aromatic carbocyclic ring or the like; and Ar 2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

  本发明揭示了一种化合物，其化学式为（I）：其中R1和R2分别代表氢原子、低碳烷基或类似物；X1、X2和X3分别代表亚甲基基团或氮原子；Y1和Y3分别代表单键、—O—或类似物；Y2代表低碳烷基基团或类似物；W1至W4独立地代表单键、亚甲基基团或类似物；L代表单键、亚甲基基团或类似物；Z1和Z2独立地代表单键、C1-4烷基基团或类似物；Ar1代表芳香环烷基环或类似物；Ar2代表双环芳香环烷基环或类似物。该化合物可用作治疗中枢疾病、心血管疾病或代谢性疾病的药物。
• Imidazopyridine Derivatives
  申请人：Kishino Hiroyuki

  公开号：US20080200494A1

  公开（公告）日：2008-08-21

  The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R 1 and R 2 may be the same or different and stand for C 1-6 alkyl or the like, R 3 and R 4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.

  该发明提供了由通式[I]表示的咪唑吡啶衍生物 [其中R1和R2可能相同或不同，且代表C1-6烷基或类似物，R3和R4代表氢原子，甲基基团或类似物，W代表单环或双环的3-8元芳香或脂肪杂环或类似物，Ar代表可选择取代的芳香杂环或类似物]。这些化合物作为黑色素浓集激素受体拮抗剂，可用于治疗中枢神经系统疾病、心血管系统疾病和代谢性疾病的药物。
• Imidazopyridine Compound
  申请人：Sakuraba Shunji

  公开号：US20070249659A1

  公开（公告）日：2007-10-25

  The present invention provides an imidazopyridine compound represented by formula (I), wherein R 1 and R 2 each independently represent a C 1-6 alkyl group et al; R 3 and R 4 each independently represent a hydrogen atom, a methyl et al; Ar 1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar 2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH 2 ) m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

  本发明提供了一种以式（I）表示的咪唑吡啶化合物，其中R1和R2各自独立地表示C1-6烷基等；R3和R4各自独立地表示氢原子、甲基等；Ar1表示一个双价的取代基，该取代基代表一个单环或双环、3-到8-成员的芳香或脂肪族杂环基等；Ar2表示一个芳香碳环基或芳香杂环基；W表示—（CH2）me等，其中m表示从0到10的整数。该化合物作为黑色素浓集激素受体拮抗剂，并且可用作肥胖症的治疗剂。
• Imidazopyridine derivatives
  申请人：Banyu Pharmaceuticals, Co., Ltd.

  公开号：US07504412B2

  公开（公告）日：2009-03-17

  The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R1 and R2 may be the same or different and stand for C1-6 alkyl or the like, R3 and R4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.

  本发明提供了由通式[I]表示的咪唑吡啶衍生物 [其中R1和R2可以相同或不同，代表C1-6烷基或类似物，R3和R4代表氢原子，甲基基团或类似物，W代表单环或双环3-8成员的芳香或脂肪族杂环或类似物，Ar代表可选取代的芳香杂环或类似物]。这些化合物作为黑素浓聚激素受体拮抗剂，并且可用于治疗中枢神经系统疾病、心血管系统疾病和代谢性疾病的药物。
• Imidazopyridine compound
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US07566781B2

  公开（公告）日：2009-07-28

  The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

  本发明提供了一种由式(I)表示的咪唑吡啶化合物，其中R1和R2各自独立地表示C1-6烷基等；R3和R4各自独立地表示氢原子、甲基等；Ar1表示一个双价取代基，代表单环或双环、3-8成员芳香族或脂环异构体基等；Ar2表示一个芳香族碳环基或芳香族异环基；W表示-（CH2）m等，其中m表示0至10的整数。该化合物作为黑色素浓集激素受体拮抗剂，并且可用作治疗肥胖症的药物。