(+)-N,alpha-二甲基苯乙胺盐酸盐 | 826-10-8

• 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: (+)-N,alpha-二甲基苯乙胺盐酸盐
• 中文别名: 8-[(4-羟基苯基)偶氮]-5-[[4-[(4-硝基-2-磺酸根苯基)氨基]苯基]偶氮]萘磺化二钠；D-甲基苯丙胺盐酸盐；D-甲基苯丙胺 盐酸盐
• 英文名称: D-methamphetamine hydrochloride
• 英文别名: (R)-(-)-methamphetamine hydrochloride；(-)-methamphetamine hydrochloride；N-methyl-1-phenylpropan-2-aminium chloride；methyl-[(2R)-1-phenylpropan-2-yl]azanium;chloride
• CAS: 826-10-8
• 化学式: C₁₀H₁₅N*ClH
• 分子量: 185.697
• InChiKey: TWXDDNPPQUTEOV-SBSPUUFOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.26
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  12
• 氢给体数：
  2
• 氢受体数：
  1

安全信息

• 储存条件：
  -20°C，密闭保存，并保持干燥。

制备方法与用途

methamphetamine (hydrochloride)是一种分类为苯丙胺类的分析标准物质。

反应信息

• 作为反应物：
  描述：

  (+)-N,alpha-二甲基苯乙胺盐酸盐 、 3-溴丙炔 在 potassium carbonate 作用下， 以 甲苯 、 乙腈 为溶剂， 反应 3.0h， 以85%的产率得到司来吉兰 盐酸盐
  参考文献：
  名称：

  A short enantioselective synthesis of ephedrine, amphetamine and their analogues via two stereocentered Co(III)-catalyzed hydrolytic kinetic resolution of racemic syn-benzyloxy epoxide

  摘要：

  An efficient route for the synthesis of 6 drugs belonging to phenethylamine and amphetamine classes in excellent overall yields and high optical purity has been described. The strategy involves introduction of stereogenic centers by means of two-stereocentered Co(III)-catalyzed hydrolytic kinetic resolution (HKR) of racemic syn-benzyloxy epoxide followed by Pd-catalyzed regioselective cationic hydrogenation of amino alcohols as the key reactions. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2015.10.010
• 作为产物：
  描述：

  盐酸司来吉兰 在 phosphate buffer 作用下， 生成 (+)-N,alpha-二甲基苯乙胺盐酸盐
  参考文献：
  名称：

  司来吉兰的痕量分解。最坏情况动力学用于稳定药物的应用

  摘要：

  1年后分析发现，HPLC测定发现司来吉兰盐酸参考标准溶液在制备时不含可检测到的杂质，该溶液在甲基苯丙胺部位含有痕量化合物。将司来吉兰溶液在pH 7和105摄氏度下加热产生的甲基苯丙胺为主要产物，其速率与一阶速率方程密切相关。仅使用这些数据和最坏情况的假设，就可以估算出各种温度下的速率常数。活化能估计为约25 kcal，并确认了所用测定法的稳定性指示有效性。司来吉兰的降解速度可忽略不计。

  DOI：

  10.1002/jps.2600830913

文献信息

• [EN] SUBSTITUTED PIPERIDINE COMPOUND AND USE THEREOF<br/>[FR] COMPOSÉ DE PIPÉRIDINE SUBSTITUÉE ET SON UTILISATION
  申请人：TAKEDA PHARMACEUTICALS CO

  公开号：WO2017135306A1

  公开（公告）日：2017-08-10

  Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.

  提供的是一种替代哌啶化合物，具有促进俐克脑肽2型受体激动剂活性。公式（I）所代表的化合物：其中每个符号如描述中所述，或其盐具有促进俐克脑肽2型受体激动剂活性，并且可用作嗜睡症的预防或治疗药物。
• HETEROCYCLIC COMPOUND AND USE THEREOF
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US20210198240A1

  公开（公告）日：2021-07-01

  The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

  本发明提供了一种具有orexin类型2受体激动剂活性的杂环化合物。 表示为公式(I)的化合物： 其中每个符号如说明书中所述，或其盐具有orexin类型2受体激动剂活性，并且可用作预防或治疗发作性嗜睡症的药剂。
• [EN] DEUTERATED MORPHINAN COMPOUNDS FOR USE IN TREATING AGITATION<br/>[FR] COMPOSÉS DE MORPHINANE DEUTÉRÉ POUR LE TRAITEMENT DE L'AGITATION
  申请人：CONCERT PHARMACEUTICALS INC

  公开号：WO2017020014A1

  公开（公告）日：2017-02-02

  This invention relates to methods of treating agitation comprising administering a morphinan compound or a pharmaceutically acceptable salt thereof. This invention also provides the use in methods of treating agitation and related disorders with such a morphinan compound in combination with quinidine, or pharmaceutically acceptable salt of either or both thereof.

  这项发明涉及治疗激动的方法，包括给予吗啡喃化合物或其药用可接受的盐。此发明还提供了在治疗激动和相关障碍的方法中使用这种吗啡喃化合物与奎尼丁或两者的药用可接受的盐的组合。
• Narcotic-NSAID ion pairs
  申请人：Sancilio D. Frederick

  公开号：US20050203115A1

  公开（公告）日：2005-09-15

  The present invention provides an ion pair compound of the formula [narcotic] + [A] − , wherein [narcotic] + represents at least one cation of at least one narcotic agent or one or more stereochemical isomers thereof and [A] − represents at least one anion of at least one NSAID or one or more stereochemical isomers thereof. An example of the ion pair compound is propoxyphene diclofenate. The ion pair compounds, or their pharmaceutical compositions, are useful in methods of treating a wide variety of conditions that indicate analgesics, anti-inflammatory agents, or both. Under the conditions prescribed for their use, the ion pair compounds exhibit poor or complete insolubility but excellent chemical stability in low pH environments, such as those found in the stomach. The ion pair compounds readily dissolve and dissociate in higher pH environments such as the small intestine to release the constituent narcotic and NSAID.

  本发明提供了一种公式为[narcotic]+[A]−的离子对化合物，其中[narcotic]+代表至少一个麻醉剂或其一个或多个立体化学异构体的至少一个阳离子，而[A]−代表至少一个非甾体抗炎药（NSAID）或其一个或多个立体化学异构体的至少一个阴离子。离子对化合物的一个例子是丙氧芬双氯芬酸。这些离子对化合物或其药物组合物在治疗表明需要镇痛剂、抗炎剂或两者都需要的方法中是有用的。在规定的使用条件下，离子对化合物在低pH环境中表现出较差或完全不溶性，但在胃中这类环境中却具有极佳的化学稳定性。离子对化合物在较高pH值的环境中，如小肠，能够快速溶解和离解，以释放组成的麻醉剂和非甾体抗炎药。
• Heterocyclic Compound
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US20180155333A1

  公开（公告）日：2018-06-07

  The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

  本发明提供了一种具有促醒素受体拮抗活性的化合物，预计可用作药物，如预防或治疗睡眠障碍、抑郁症、焦虑症、恐慌症、精神分裂症、药物依赖、阿尔茨海默病等的药剂。 本发明涉及由以下式（I）表示的化合物： 其中每个符号如规范中定义，或其盐。