lespedamine | 4335-93-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: lespedamine
• 英文别名: 2-(1-methoxyindol-3-yl)-N,N-dimethylethanamine
• CAS: 4335-93-7
• 化学式: C₁₃H₁₈N₂O
• 分子量: 218.299
• InChiKey: DXTZTYQDNUHCAB-UHFFFAOYSA-N

物化性质

• 沸点：
  100-106 °C(Press: 0.08 Torr)
• 密度：
  1.03±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  17.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  三甲基氯硅烷 、 lespedamine 在 正丁基锂 作用下， 生成 3-(dimethylaminoethyl)-1-methoxy-2-(trimethylsilyl)indole
  参考文献：
  名称：

  Nakagawa, Kyoko; Somei, Masanori, Heterocycles, 1994, vol. 39, # 1, p. 31 - 34

  摘要：

  DOI：
• 作为产物：
  描述：

  N,N-二甲基色胺 在 三乙基硅烷 、 sodium tungstate 、 双氧水 、 三氟乙酸 作用下， 以 甲醇 、 水 为溶剂， 反应 4.5h， 生成 lespedamine
  参考文献：
  名称：

  The Chemistry of Indoles. CIII. Simple Syntheses of Serotonin, N-Methylserotonin, Bufotenine, 5-Methoxy-N-methyltryptamine, Bufobutanoic Acid, N-(Indol-3-yl)methyl-5-methoxy-N-methyltryptamine, and Lespedamine Based on 1-Hydroxyindole Chemistry.

  摘要：

  本文描述了利用1-羟色胺的选择性亲核取代反应，合成新型简单物质的方法，这些物质包括：血清素（1a）、N-甲基血清素（1b）、蟾毒色胺（1c）、5-甲氧基-N-甲基色胺（2a）、蟾毒色酸（3a）、N-(吲哚-3-基)甲基-5-甲氧基-N-甲基色胺（4）和莱斯佩达明（5）。此外，还报道了有效的5-苄氧基色胺和1-甲氧基-2-氧吲哚合成方法。

  DOI：

  10.1248/cpb.49.87

文献信息

• Pyrrolo {2,1-b}{1,3}benzothiazepines with atypical antipsychotic activity
  申请人：——

  公开号：US20020006921A1

  公开（公告）日：2002-01-17

  Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) 1 where the groups are defined as in the description are disclosed. As compared to known antipsychotic agents, these compounds present substantial activity associated with a simultaneous reduction in unwanted extrapyramidal symptoms. These compounds can be formulated in pharmaceutical compositions for the treatment of psychoses such as, for example, schizophrenia.

  本发明公开了具有吡咯[2,1-b][1,3]苯并噻吩结构的聚缩杂环化合物，其化学式如下（I）1，其中所述基团的定义如说明书所述。与已知的抗精神病药物相比，这些化合物呈现出与同时减少不良的锥体外症状相关的显著活性。这些化合物可以制成药物组合物，用于治疗精神病，例如精神分裂症。
• Electrically heated aerosol delivery system
  申请人：PHILIP MORRIS PRODUCTS S.A.

  公开号：US10721963B2

  公开（公告）日：2020-07-28

  An aerosol delivery system for delivering aerosolised medicament particles to a user is provided, including a cartridge and a device configured to receive the cartridge. The cartridge includes a first compartment including a delivery enhancing compound source; a second compartment including a medicament source; a vaporiser configured to heat the medicament; and a transfer element configured to convey the medicament from the second compartment to the vaporiser. The device includes an outer housing; a power source; a temperature controller configured to control the temperature of the first compartment; and electronic circuitry configured to control power to the temperature controller from the power source. The electronic circuitry is configured to maintain the first compartment at a temperature of between about 30° C. and about 50° C.

  本发明提供了一种气溶胶给药系统，用于向用户提供气溶胶化的药物颗粒，该系统包括一个药盒和一个配置为接收该药盒的装置。药盒包括第一隔室，其中包括递送增强化合物源；第二隔室，其中包括药剂源；蒸发器，配置用于加热药剂；以及传送元件，配置用于将药剂从第二隔室传送到蒸发器。该装置包括一个外壳；一个电源；一个温度控制器，配置用于控制第一隔室的温度；以及电子电路，配置用于控制从电源向温度控制器供电。电子电路被配置为将第一隔室的温度保持在约 30°C 至约 50°C 之间。
• Aerosol-generating system comprising a bimetallic strip
  申请人：Philip Morris Products S.A.

  公开号：US10750785B2

  公开（公告）日：2020-08-25

  An aerosol-generating system is provided, including an aerosol-generating device including a heater element; an aerosol-generating article including a medicament source and a volatile delivery enhancing compound source; a bimetallic strip provided in the aerosol-generating device or the aerosol-generating article, the bimetallic strip including a first end in thermal contact with the heater element and a second end in thermal contact with the volatile delivery enhancing compound source, the bimetallic strip being configured so that heating the first end of the bimetallic strip above a predetermined temperature results in displacement of the first end of the bimetallic strip away from the heater element.

  提供了一种气溶胶产生系统，包括气溶胶产生装置，其中包括加热器元件；气溶胶产生物品，其中包括药源和挥发性输送增强化合物源；气溶胶产生装置或气溶胶产生物品中的双金属带，双金属带包括与加热器元件热接触的第一端和与挥发性输送增强化合物源热接触的第二端，双金属带被配置成使双金属带的第一端加热到预定温度以上导致双金属带的第一端远离加热器元件。
• Resealable aerosol-generating article
  申请人：Philip Morris Products S.A.

  公开号：US10786007B2

  公开（公告）日：2020-09-29

  An aerosol-forming article is provided, including an airflow inlet and an airflow outlet; a medicament source and a volatile delivery enhancing compound source disposed between the airflow inlet and the airflow outlet, and a moveable portion moveable between an open position in which the medicament source and the volatile delivery enhancing compound source are in fluid communication with both the airflow inlet and the airflow outlet, and a closed position in which each of the medicament source and the volatile delivery enhancing compound source is in communication with only one or none of the airflow inlet and the airflow outlet.

  提供了一种气溶胶成型品，包括气流入口和气流出口；设置在气流入口和气流出口之间的药剂源和挥发性输送增强化合物源，以及可在药剂源和挥发性输送增强化合物源与气流入口和气流出口均处于流体连通状态的打开位置和药剂源和挥发性输送增强化合物源仅与气流入口和气流出口中的一个或任何一个连通的关闭位置之间移动的可移动部分。
• Aerosol-generating system comprising a resilient member
  申请人：Philip Morris Products S.A.

  公开号：US10806873B2

  公开（公告）日：2020-10-20

  An aerosol-generating system is provided, including an aerosol-generating device including a heater element; an aerosol-generating article, including a medicament source and a volatile delivery enhancing compound source; and at least one resilient member provided in the aerosol-generating device or the aerosol-generating article and being resiliently biased against the heater element, wherein at least one of the medicament source and the volatile delivery enhancing compound source contacts the at least one resilient member, and the aerosol-generating system is configured to heat the medicament source and the volatile delivery enhancing compound source of the aerosol-generating article so that the medicament source has a higher temperature than that of the volatile delivery enhancing compound source.

  提供了一种气溶胶产生系统，包括一个气溶胶产生装置，其中包括一个加热器元件；一个气溶胶产生装置，其中包括一个药源和一个挥发性给药增强化合物源；气溶胶发生装置或气溶胶发生装置中设置的至少一个弹性部件，该部件与加热器元件弹性偏置，其中药源和挥发性给药增强化合物源中的至少一个与至少一个弹性部件接触，气溶胶发生系统被配置为加热气溶胶发生装置的药源和挥发性给药增强化合物源，使药源的温度高于挥发性给药增强化合物源的温度。