4-(3-bromopropoxy)benzenesulfonyl chloride | 138557-92-3

• 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-(3-bromopropoxy)benzenesulfonyl chloride
• 英文别名: 4-(3-bromopropoxy)benzene-1-sulfonyl chloride；4-(3-bromopropoxy)benzenesulfonic acid chloride；1-bromo-3-(4-chlorosulfonylphenoxy)propane
• CAS: 138557-92-3
• 化学式: C₉H₁₀BrClO₃S
• 分子量: 313.6
• InChiKey: BHAOZXDFDRKMON-UHFFFAOYSA-N

物化性质

• 沸点：
  414.8±25.0 °C(Predicted)
• 密度：
  1.597±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(3-bromopropoxy)benzenesulfonyl chloride 在 氨 、 sodium hydroxide 作用下， 以 乙醇 、 二氯甲烷 、 丙酮 为溶剂， 反应 24.92h， 生成 1-isopropyl-3-[4-(3-pyrrolidin-1-ylpropoxy)benzene]sulfonylurea
  参考文献：
  名称：

  Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies

  摘要：

  The combination of antagonism at histamine H-3 receptor and the stimulation of insulin secretion have been proposed as an approach to new dual therapeutic agents for the treatment of type 2 diabetes mellitus associated with obesity. We have designed and synthesized a new series of non-imidazole derivatives, based on a basic amine ring connected through an alkyl spacer of variable length to a phenoxysulfonylurea moiety. These compounds were initially evaluated for histamine H-3 receptor binding affinities, suggesting that a propoxy chain linker between the amine and the core ring could be essential for optimal binding affinity. Compound 56, 1-(naphthalen-1-yl)-3-[(p-(3-pyrrolidin-1-ylpropoxy) benzene)]sulfonylurea exhibited the best H-3 antagonism affinity. However, since all these derivatives failed to block K-ATP channels, the link of these two related moieties should not be considered a good pharmacophore for obtaining new dual H-3 antagonists with insulinotropic activity, suggesting the necessity to propose a new chemical hybrid prototype. (C)2012 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2012.02.049
• 作为产物：
  描述：

  3-苯氧基溴丙烷 在 氯磺酸 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以38%的产率得到4-(3-bromopropoxy)benzenesulfonyl chloride
  参考文献：
  名称：

  [EN] NOVEL COMPOUND, PREPARATION METHOD THEREOF, AND USE THEREOF
  [FR] NOUVEAU COMPOSÉ, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION

  摘要：

  本发明涉及一种制备具有选择性功能化酪氨酸的生物材料的方法，具有选择性功能化酪氨酸的生物材料，以及含有该生物材料作为活性成分的药物组合物。本发明的一种制备生物材料的方法，其中将由式2表示的化合物偶联到生物材料，使得该化合物能够选择性地偶联到酪氨酸，且在生物材料中的产率较高，酪氨酸位于水溶液表面，使得其与酪氨酸以外的氨基酸不发生偶联，当只有一个酪氨酸存在时，不会出现异质混合物，同时保持生物材料的固有活性，因此该化合物可以有效地用作含有生物材料药物的药物组合物的活性成分。此外，该方法可以选择性功能化酪氨酸，因此可以有效地用于生物材料中的酪氨酸功能化。

  公开号：

  WO2021145729A1

文献信息

• Pyrimidinedione derivatives and antiarrhythmic agents containing same
  申请人：Mitsui Toatsu Chemicals, Incorporated

  公开号：US05332739A1

  公开（公告）日：1994-07-26

  Pyrimidinedione derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 is so linked with each other as to make an alkylene chain and thus form a heterocyclic structure, A, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.3 are substituents, respectively, and n is 2 or 3 have a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain and a heterocyclic ring having two nitrogen atoms. These compounds are useful for a medical treatment of cardiac arrhythmias.

  Pyrimidinedione衍生物的化学式为：##STR1## 其中R.sup.1和R.sup.2通过一个烷基链相连，从而形成一个杂环结构，A，R.sup.3，R.sup.4，X.sup.1，X.sup.2和X.sup.3分别是取代基，n为2或3，具有一个基本骨架，其中苯基部分和嘧啶二酮部分通过一个包含一个烷基链和一个含有两个氮原子的杂环环的结构相连。这些化合物对于治疗心律失常很有用。
• [EN] ARYLOXYALKYLAMINE DERIVATES AS H3 RECEPTOR LIGANDS<br/>[FR] DERIVES D'ARYLOXYALKYLAMINE TELS QUE DES LIGANDS DU RECEPTEUR H3
  申请人：GLAXO GROUP LTD

  公开号：WO2004037800A1

  公开（公告）日：2004-05-06

  The present invention relates to novel benzyloxy derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

  本发明涉及具有药理活性的新型苄氧基衍生物，其制备方法，含有它们的组合物以及它们在治疗神经系统和精神疾病中的用途。
• [EN] NOVEL COMPOUND, PREPARATION METHOD THEREOF, AND USE THEREOF<br/>[FR] NOUVEAU COMPOSÉ, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
  申请人：DAEGU GYEONGBUK MEDICAL INNOVATION FOUND

  公开号：WO2021145729A1

  公开（公告）日：2021-07-22

  The present invention relates to a method for preparing a biomaterial having selectively functionalized tyrosine, a biomaterial having selectively functionalized tyrosine, and a pharmaceutical composition containing the same as an active ingredient. The method for preparing a biomaterial to which a compound represented by formula 2 is coupled, of the present invention, allows the compound represented by formula 2 to be selectively coupled, in a high yield in a biomaterial, to tyrosine, which is present on the surface of an aqueous solution such that the coupling thereof to amino acids other than tyrosine does not occur and, when only one tyrosine is present, heterogeneous mixtures are not present and the inherent activity of the biomaterial is maintained, and thus the compound can be effectively used as a pharmaceutical composition containing a biomaterial drug as an active ingredient. In addition, the method can selectively functionalize tyrosine, and thus can be effectively used for tyrosine functionalization in a biomaterial.

  本发明涉及一种制备具有选择性功能化酪氨酸的生物材料的方法，具有选择性功能化酪氨酸的生物材料，以及含有该生物材料作为活性成分的药物组合物。本发明的一种制备生物材料的方法，其中将由式2表示的化合物偶联到生物材料，使得该化合物能够选择性地偶联到酪氨酸，且在生物材料中的产率较高，酪氨酸位于水溶液表面，使得其与酪氨酸以外的氨基酸不发生偶联，当只有一个酪氨酸存在时，不会出现异质混合物，同时保持生物材料的固有活性，因此该化合物可以有效地用作含有生物材料药物的药物组合物的活性成分。此外，该方法可以选择性功能化酪氨酸，因此可以有效地用于生物材料中的酪氨酸功能化。
• 1-benzenesulfonyl-1-1,3-dihydroindol-2-one derivatives, their
  申请人：Sanofi

  公开号：US05849780A1

  公开（公告）日：1998-12-15

  The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.

  这项发明涉及公式为##STR1##的1-苯磺酰基-1,3-二氢吲哚-2-酮衍生物及其盐，适当情况下涉及它们的制备以及它们存在的药物组合物。这些化合物对加压素和/或催产素受体具有亲和力。
• Aryloxyalkylamine derivatives as h3 receptor ligands
  申请人：Best John Desmond

  公开号：US20060052597A1

  公开（公告）日：2006-03-09

  The present invention relates to novel benzyloxy derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

  本发明涉及具有药理活性的新型苯甲氧基衍生物，其制备过程，包含它们的组合物以及它们在治疗神经病学和精神病学疾病中的应用。