舒洛昔芬 | 25827-12-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 舒洛昔芬
• 中文别名: 二苯磺酰乙胺
• 英文名称: N-(N’,N’-diethylamino)-S,S-diphenylsulfoximine
• 英文别名: suloxifen；N-(2-Diaethylamino-aethyl)-S,S-diphenyl-sulfoximin-14C)>；N-(2-Diaethylamino-aethyl)-S,S-diphenyl-sulfoximin-(1-¹⁴C)；N-(2-Diaethylamino-aethyl)-S,S-diphenyl-sulfoximin；N,N-Diaethylaminoaethyl-S,S-diphenyl-sulfoxim；N-(2-Diaethylamino-aethyl)-S,S-diphenyl-sulfoximin-(Phenyl-(U-¹⁴C))；N,N-diethyl-2-[[oxo(diphenyl)-λ6-sulfanylidene]amino]ethanamine
• CAS: 25827-12-7
• 化学式: C₁₈H₂₄N₂OS
• 分子量: 316.467
• InChiKey: HSOWGTFAGFRXKH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  41
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  硫酸二乙酯 、 舒洛昔芬 以 乙腈 为溶剂， 生成 N,N,N-triethyl-2-((oxodiphenyl-l6-sulfaneylidene)amino)ethan-1-aminium ethyl sulfate
  参考文献：
  名称：

  Satzinger; Stoss, Arzneimittel-Forschung/Drug Research, 1970, vol. 20, # 9, p. 1214 - 1217

  摘要：

  DOI：
• 作为产物：
  描述：

  二苯砜 在 sodium azide 、 PPA 作用下， 生成 舒洛昔芬
  参考文献：
  名称：

  Satzinger; Stoss, Arzneimittel-Forschung/Drug Research, 1970, vol. 20, # 9, p. 1214 - 1217

  摘要：

  DOI：

文献信息

• <i>N</i>-Alkylations of<i>N</i>H-Sulfoximines and<i>N</i>H-Sulfondiimines with Alkyl Halides Mediated by Potassium Hydroxide in Dimethyl Sulfoxide
  作者：Christine M. M. Hendriks、Rebekka A. Bohmann、Marina Bohlem、Carsten Bolm

  DOI：10.1002/adsc.201400193

  日期：2014.5.26

  A general method for the N‐alkylation of NH‐sulfoximines and NH‐sulfondiimines has been developed, employing alkyl bromides with KOH in DMSO at room temperature. A variety of previously inaccessible N‐alkylated sulfoximines and sulfondiimines was prepared in good to excellent yields (up to 97%). As an application, the conditions were used to access the biologically active Suloxifen.

  对于一般方法Ñ的烷基化Ñ H-亚磺酰亚胺和Ñ H-sulfondiimines已经开发，采用用KOH烷基溴化物在DMSO在室温下。制备了许多以前无法获得的N烷基化亚砜亚砜和磺二亚胺，收率高达97％。作为应用，使用条件来获得具有生物活性的舒洛昔芬。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Process for the preparation of especially pharmacologically active compounds containing a sulfoxide group
  申请人：ZAMBON S.p.A.

  公开号：EP0125654A2

  公开（公告）日：1984-11-21

  Process for the preparation of compounds containing a sulfoxide group by oxidation of a thioether with hypochlorite in an alkaline medium at a pH higher than 10 and at a temperature from 0° to 40°C.

  在 pH 值大于 10 和温度为 0° 至 40°C 的碱性介质中，用次氯酸盐氧化硫醚，制备含有亚砜基团的化合物的工艺。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。