6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-2-(toluene-4-sulfonyl)-1,2,3,4-tetrahydro-isoquinoline | 1350377-10-4

• 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: 6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-2-(toluene-4-sulfonyl)-1,2,3,4-tetrahydro-isoquinoline
• 英文别名: 6-((2S,3'S)-2-methyl[1,3']bipyrrolidinyl-1'-yl)-2-(toluene-4-sulfonyl)-1,2,3,4-tetrahydroisoquinoline；2-(4-methylphenyl)sulfonyl-6-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]-3,4-dihydro-1H-isoquinoline
• CAS: 1350377-10-4
• 化学式: C₂₅H₃₃N₃O₂S
• 分子量: 439.622
• InChiKey: XYXJBZURYUBRDB-RDPSFJRHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  52.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-2-(toluene-4-sulfonyl)-1,2,3,4-tetrahydro-isoquinoline 在 三乙胺 、 红铝 作用下， 以 二氯甲烷 、 甲苯 为溶剂， 生成 (4-methoxy-phenyl)-[6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-3,4-dihydro-1H-isoquinolin-2-yl]-methanone
  参考文献：
  名称：

  [EN] SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
  [FR] DÉRIVÉS N-ALKYL ET N-ACYL TÉTRAHYDRO-ISOQUINOLINE SUBSTITUÉS, PROCÉDÉ DE PRÉPARATION ET APPLICATION THÉRAPEUTIQUES ASSOCIÉS

  摘要：

  本发明揭示并声明了一系列式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物。其中R、R1、R2、X、m、n和p如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此在制药剂中特别有用，尤其是在治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还揭示了制备式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。

  公开号：

  WO2011143145A1
• 作为产物：
  描述：

  N-(3-bromophenethyl)-4-methylbenzenesulfonamide 在 tris-(dibenzylideneacetone)dipalladium(0) 、 硫酸 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 sodium t-butanolate 作用下， 以 乙二醇二甲醚 、 甲苯 为溶剂， 反应 15.0h， 生成 6-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-2-(toluene-4-sulfonyl)-1,2,3,4-tetrahydro-isoquinoline
  参考文献：
  名称：

  [EN] SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
  [FR] DÉRIVÉS N-ALKYL ET N-ACYL TÉTRAHYDRO-ISOQUINOLINE SUBSTITUÉS, PROCÉDÉ DE PRÉPARATION ET APPLICATION THÉRAPEUTIQUES ASSOCIÉS

  摘要：

  本发明揭示并声明了一系列式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物。其中R、R1、R2、X、m、n和p如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此在制药剂中特别有用，尤其是在治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还揭示了制备式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。

  公开号：

  WO2011143145A1

文献信息

• [EN] SUBSTITUTED N-HETEROARYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF<br/>[FR] DÉRIVÉS DE N-HÉTÉROARYL TÉTRAHYDRO-ISOQUINOLINES SUBSTITUÉES, PROCÉDÉ DE PRÉPARATION ET USAGE THÉRAPEUTIQUE ASSOCIÉS
  申请人：SANOFI SA

  公开号：WO2011143155A1

  公开（公告）日：2011-11-17

  The present invention discloses and claims a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of Formula (I). Wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of Formula (I) and intermediates therefor.

  本发明公开并声明了一系列Formula (I)的N-杂环芳基四氢异喹啉衍生物。其中R、R1、R2、X、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在制药剂中特别有用，特别是在治疗和/或预防多种由H3受体调节的疾病中，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备Formula (I)的N-杂环芳基四氢异喹啉衍生物及其中间体的方法。
• SUBSTITUTED N-HETEROARYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：Sanofi

  公开号：US20130059838A1

  公开（公告）日：2013-03-07

  The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R 1 , R 2 , X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本公开涉及一系列代替的N-杂环芳基四氢异喹啉衍生物，其化学式为(I)，其中R、R1、R2、X、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种H3受体调节的疾病中，特别是作为药物剂量是有用的。此外，本公开还涉及制备代替的N-杂环芳基四氢异喹啉衍生物的方法和中间体。
• SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：SANOFI

  公开号：US20130065919A1

  公开（公告）日：2013-03-14

  The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R 1 , R 2 , X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本公开涉及一系列式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物，其中R、R1、R2、X、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种受H3受体调节的疾病中，特别有用作为药物制剂。此外，本公开还涉及制备式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。
• Substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof
  申请人：Sanofi

  公开号：US08871788B2

  公开（公告）日：2014-10-28

  The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本公开涉及一系列公式（I）的取代N-烷基和N-酰基四氢异喹啉衍生物，其中R、R1、R2、X、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在治疗和/或预防多种由H3受体调节的疾病，包括与中枢神经系统相关的疾病方面，作为药物剂量是有用的。此外，本公开还涉及制备公式（I）的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。
• Substituted N-heteroaryl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof
  申请人：Sanofi

  公开号：US08623877B2

  公开（公告）日：2014-01-07

  The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本公开涉及一系列代替N-杂环芳基四氢异喹啉衍生物的化合物，其化学式为（I），其中R，R1，R2，X，m，n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种H3受体调节的疾病方面，特别有用作为药物剂。此外，本公开还涉及制备代替N-杂环芳基四氢异喹啉衍生物的方法以及其中间体。