4-Difluoromethoxy-N-[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-benzenesulfonamide | 1149659-86-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 4-Difluoromethoxy-N-[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-benzenesulfonamide
• 英文别名: 4-(difluoromethoxy)-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]benzenesulfonamide
• CAS: 1149659-86-8
• 化学式: C₁₉H₂₃F₂N₃O₄S
• 分子量: 427.472
• InChiKey: FRAYZRIMQVZJAQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  79.5
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  4-(二氟甲氧基)苯磺酰氯 、 1-(5-氨基-2-甲氧基苯基)-4-甲基哌嗪 在 甲苯 、 二氯甲烷 、 氯化铵 、 氯化钠 、 Sodium sulfate-III 、 crude product 作用下， 以 吡啶 为溶剂， 反应 16.0h， 以to yield 0.395 g of the desired title compound的产率得到4-Difluoromethoxy-N-[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-benzenesulfonamide
  参考文献：
  名称：

  BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR

  摘要：

  本发明涉及公式 I 和 I' 的新型苯磺酰苯胺化合物及其生理耐受的酸加成盐和 N-氧化物。这些化合物具有有价值的治疗特性，特别适用于治疗对5-羟色胺5-HT6受体调节有反应的疾病。 其中，R1为氢或甲基，R2为氢或甲基，R3为氢、氟、C1-C2烷氧基或氟代C1-C2烷氧基；R4为氢、C1-C4烷基或氟代C1-C4烷基；R5为氢、氟、C1-C2烷基、氟代C1-C2烷基、C1-C2烷氧基或氟代C1-C2烷氧基；R6为氢、氟和氯。

  公开号：

  US20110086863A1

文献信息

• Benzenesulfonanilide compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
  申请人：Abbott GmbH & Co. KG

  公开号：US07790727B2

  公开（公告）日：2010-09-07

  The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.

  本发明涉及公式I和I'的新型苯磺酰胺化合物及其生理耐受的酸加成盐和其N-氧化物。该化合物具有有价值的治疗特性，尤其适用于治疗对5-羟色胺5-HT6受体调节有反应的疾病。 其中， R1为氢或甲基； R2为氢或甲基； R3为氢、氟、C1-C2烷氧基或氟代C1-C2烷氧基； R4为氢、C1-C4烷基或氟代C1-C4烷基； R5为氢、氟、C1-C2烷基、氟代C1-C2烷基、C1-C2烷氧基或氟代C1-C2烷氧基； R6为氢、氟或氯。
• US7790727B2
  申请人：——

  公开号：US7790727B2

  公开（公告）日：2010-09-07
• [EN] BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR<br/>[FR] COMPOSÉS DE BENZÈNESULFONANILIDE ADAPTÉS AU TRAITEMENT DE TROUBLES RÉPONDANT À LA MODULATION DU RÉCEPTEUR SÉROTONINERGIQUE 5-HT6
  申请人：ABBOTT GMBH & CO KG

  公开号：WO2009056632A1

  公开（公告）日：2009-05-07

  The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.
• BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
  申请人：Braje Wilfried Martin

  公开号：US20090131452A1

  公开（公告）日：2009-05-21

  The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. wherein R 1 is hydrogen or methyl R 2 is hydrogen or methyl R 3 hydrogen, fluorine C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; R 4 is hydrogen, C 1 -C 4 alkyl or fluorinated C 1 -C 4 alkyl; R 5 is hydrogen, fluorine, C 1 -C 2 alkyl fluorinated C 1 -C 2 alkyl C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; and R 6 is hydrogen, fluorine or chlorine.

  本发明涉及新型苯磺酰苯胺化合物I和I′的化学式，以及其生理耐受的酸盐和N-氧化物。这些化合物具有有价值的治疗特性，特别适用于治疗对调节5-羟色胺5-HT6受体有响应的疾病。其中R1是氢或甲基，R2是氢或甲基，R3是氢、氟、C1-C2烷氧基或氟化C1-C2烷氧基；R4是氢、C1-C4烷基或氟化C1-C4烷基；R5是氢、氟、C1-C2烷基、氟化C1-C2烷基、C1-C2烷氧基或氟化C1-C2烷氧基；R6是氢、氟或氯。