4-benzyl-2-toluene-p-sulphnyloxymethylmorpholine | 40987-53-9

• 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-benzyl-2-toluene-p-sulphnyloxymethylmorpholine
• 英文别名: (4-benzylmorpholin-2-yl)methyl 4-methyl benzenesulfonate；4-benzyl-2-(toluene-p-sulphonyloxymethyl)morpholine；2-tosyloxymethyl-4-benzylmorpholine；2-(p-toluenesulfonyloxymethyl)-4-benzylmorpholine；4-benzyl-2-(toluene-4-sulfonyloxymethyl)-morpholine；4-benzyl-2-(p-toluenesulfonyloxymethyl)morpholine；R,S-2-tosyloxymethyl-4-benzylmorpholine；4-Benzyl-2-toluene-p-sulphonyloxymethylmorpholine；(4-benzylmorpholin-2-yl)methyl 4-methylbenzenesulfonate
• CAS: 40987-53-9
• 化学式: C₁₉H₂₃NO₄S
• 分子量: 361.462
• InChiKey: KYOBGUIFQMOUAX-UHFFFAOYSA-N

物化性质

• 沸点：
  501.4±35.0 °C(Predicted)
• 密度：
  1.218±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  64.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-benzyl-2-toluene-p-sulphnyloxymethylmorpholine 在 palladium on activated charcoal 氢气 、 溶剂黄146 作用下， 反应 3.0h， 以57%的产率得到Toluene-4-sulfonic acid morpholin-2-ylmethyl ester
  参考文献：
  名称：

  (R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl]morpholine Methanesulfonate:  A New Selective Rat 5-Hydroxytryptamine_1B Receptor Antagonist

  摘要：

  In the search for new 5-hydroxytryptamine (5-HT) receptor antagonists it was found that the compound (R)-(+)-2-[[[3-(morpholinomethyl)-2H-chromen-8-yl]oxy]methyl]morpholine methanesulfonate, (R)-25, is a selective rat 5-hydroxytryptamine(1B) (r5-HT1B) receptor antagonist. The binding profile showed a 13-fold preference for r5-HT1B (K-i = 47 +/- 5 nM; n = 3) vs bovine 5-HT1B (K-i = 630 nM; n = 1) receptors. The compound had very low affinity for other monoaminergic receptors examined. The r5-HT1B receptor antagonism was demonstrated by the potentiation of the K+-stimulated release of [H-3]-5-HT from superfused rat brain slices in vitro, an effect that was antagonized by addition of 5-HT to the superfusion fluid. (R)-25 at 20 mg/kg sc enhanced the 5-HT turnover in four rat brain regions (hypothalamus, hippocampus, striatum, and frontal cortex) with about 40% measured as the 5-HTP accumulation after decarboxylase inhibition with 3-hydroxybenzylhydrazine. At 3 mg/kg sc (R)-25 produced a significant increase in the number of wet dog shakes in rats, a 5-HT2A/5-HT2C response that was abolished by depletion of 5-HT after pretreatment with the tryptophan hydroxylase inhibitor p-chlorophenylalanine. These observations show that (R)-25, by inhibiting terminal r5-HT1B autoreceptors, increases the 5-HT turnover and the synaptic concentration of 5-HT.

  DOI：

  10.1021/jm970806i
• 作为产物：
  描述：

  4-苄基-2-(氯甲基)吗啉 在 吡啶 、 formamide 作用下， 反应 5.0h， 生成 4-benzyl-2-toluene-p-sulphnyloxymethylmorpholine
  参考文献：
  名称：

  Loftus, F., Synthetic Communications, 1980, vol. 10, # 1, p. 59 - 74

  摘要：

  DOI：

文献信息

• [EN] SUBSTITUTED HETEROCYCLIC DERIVATIVES AS GPR AGONISTS AND USES THEREOF<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES SUBSTITUÉS EN TANT QU'AGONISTES DE GPR ET LEURS UTILISATIONS
  申请人：PIRAMAL ENTPR LTD

  公开号：WO2015028960A1

  公开（公告）日：2015-03-05

  The present invention generally relates to substituted heterocyclic derivatives (the compounds of Formula (I)), processes for their preparation, pharmaceutical compositions containing said compounds, their use as G-protein coupled receptor (GPR) agonists, particularly as GPR40 agonists and methods of using these compounds in the treatment of GPR40 mediated diseases or conditions such as Type 2 diabetes, obesity, dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

  本发明通常涉及取代杂环衍生物（式（I）化合物），其制备方法，含有所述化合物的药物组合物，它们作为G-蛋白偶联受体（GPR）激动剂的用途，特别是作为GPR40激动剂，并且使用这些化合物治疗GPR40介导的疾病或症状，如2型糖尿病、肥胖症、血脂异常、高脂血症、高胆固醇血症和高甘油三酯血症的方法。
• NOVEL TRIAZOLOPYRAZINE DERIVATIVE AND USE THEREOF
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：US20150259350A1

  公开（公告）日：2015-09-17

  The present invention relates to a novel triazolopyrazine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating hyper proliferative disorder. The present invention can be useful as a therapeutic agent for various hyper proliferative disorders associated with excessive cell proliferation and growth caused by abnormal kinase activity, such as cancer, psoriasis, rheumatoid arthritis, and diabetic retinopathy, by efficiently inhibiting c-Met tyrosine kinase activity.

  本发明涉及一种新型三唑吡嗪衍生物或其药用盐，以及含有该衍生物作为活性成分的药物组合物，用于预防或治疗过度增殖性疾病。本发明可以作为治疗剂，用于有效抑制c-Met酪氨酸激酶活性，从而对抗与异常激酶活性引起的细胞过度增殖和生长相关的各种过度增殖性疾病，如癌症、银屑病、类风湿性关节炎和糖尿病视网膜病变。
• Quinolinecarboxylic acid derivatives, antibacterial agent containing the
  申请人：Kanebo, Ltd.

  公开号：US05166203A1

  公开（公告）日：1992-11-24

  Novel quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein Z is ##STR2## or ##STR3## in which R.sup.1 is hydrogen atom, a halogen atom, hydroxy or a lower alkyloxy; R.sup.2 is a halogen atom, hydroxy or a lower alkyloxy; R.sup.3 is a lower alkyl; and R.sup.4 is hydroxy or a di(lower alkyl)amino, and a pharmaceutically acceptable salt thereof, which have excellent antibacterial activities and are useful as an antibacterial agent, a pharmaceutical composition containing the same, and process for preparing the same.

  新型喹啉羧酸衍生物的化学式为：##STR1## 其中 Z 为 ##STR2## 或 ##STR3##，其中 R.sup.1 为氢原子、卤原子、羟基或较低的烷氧基；R.sup.2 为卤原子、羟基或较低的烷氧基；R.sup.3 为较低的烷基；R.sup.4 为羟基或二(较低的烷基)氨基，以及其在药学上可接受的盐，具有优异的抗菌活性，可用作抗菌剂，含有相同化合物的药物组合物，以及制备相同化合物的方法。
• METHODS FOR PRODUCING VILOXAZINE SALTS AND NOVEL POLYMORPHS THEREOF
  申请人：Liang Likan

  公开号：US20110251198A1

  公开（公告）日：2011-10-13

  Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.

  这里提供了制备维洛西嗪及其各种盐的方法，以及维洛西嗪相关化合物，如新型中间反应产物和其多晶形式。具体而言，这些方法提供了维洛西嗪盐酸盐的基本纯净API，同时避免了不良杂质。这些方法进一步提供了分离、鉴定和表征维洛西嗪新型多晶形式的方法。此外，还提供了维洛西嗪新中间体的合成、鉴定和表征方法，以及一些重要代谢产物和代谢产物前体的合成方法。
• 2-(Substituted anilino) methylmorpholine compounds
  申请人：Imperial Chemical Industries Limited

  公开号：US03974156A1

  公开（公告）日：1976-08-10

  The disclosure relates to new 2-(substituted anilino)-methylmorpholine derivatives which possess sedative activity, to processes for the manufacture of the said morpholine derivatives, and to pharmaceutical compositions containing them. Typical of the morpholine derivatives disclosed is 2-(3-methoxyanilino)methylmorpholine.

  该披露涉及新的2-(取代基苯胺基)-甲基吗啡啶衍生物，具有镇静作用，以及制造所述吗啡啶衍生物的工艺和包含它们的制药组合物。披露的吗啡啶衍生物的典型代表是2-(3-甲氧基苯胺基)甲基吗啡啶。