D-盐酸司来吉兰 | 4528-51-2

• 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: D-盐酸司来吉兰
• 英文名称: D-deprenyl
• 英文别名: (+)-Deprenyl；(+)-Selegiline；(2S)-N-methyl-1-phenyl-N-prop-2-ynylpropan-2-amine
• CAS: 4528-51-2
• 化学式: C₁₃H₁₇N
• 分子量: 187.285
• InChiKey: MEZLKOACVSPNER-LBPRGKRZSA-N

物化性质

• 熔点：
  141-142 °C
• 沸点：
  130-132 °C(Press: 12 Torr)
• 密度：
  0.954±0.06 g/cm3(Predicted)
• 溶解度：
  可溶于水中

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  N-((S)-1-甲基-2-苯基乙基)甲酰胺 在 lithium aluminium tetrahydride 作用下， 生成 D-盐酸司来吉兰
  参考文献：
  名称：

  2-甲基-3-丁炔-2-醇在曼尼希反应中作为乙炔前体。单胺氧化酶自杀灭活剂的新合成。

  摘要：

  DOI：

  10.1021/jo00435a026

文献信息

• MAO Inhibitors and Their Conjugates as Therapeutics For The Treatment of Brain Cancer
  申请人：University of Southern California

  公开号：US20150209361A1

  公开（公告）日：2015-07-30

  A pharmaceutical composition and method for treating brain cancer are provided. The method includes administering to a patient in need thereof an effective amount of one or more compounds that include moclobemide, clorgyline, clorgyline's Near-infra-red dye Monoamine Oxidase Inhibitor (NMI), and MHI 148-clorgyline, and their salt thereof. The composition and method are particularly effective in reducing the size of glioblastomas that are temozolomide (TMZ) resistant.

  提供了一种用于治疗脑癌的药物组合物和方法。该方法包括向需要治疗的患者施用一种或多种化合物的有效量，其中包括莫克洛贝胺、克洛吉林、克洛吉林的近红外染料单胺氧化酶抑制剂(NMI)和MHI 148-克洛吉林及其盐。该组合物和方法特别有效于减小对替莫唑胺（TMZ）具有抵抗力的胶质母细胞瘤的大小。
• MAO inhibitors and their conjugates as therapeutics for the treatment of brain cancer
  申请人：University of Southern California

  公开号：US10561663B2

  公开（公告）日：2020-02-18

  A pharmaceutical composition and method for treating brain cancer are provided. The method includes administering to a patient in need thereof an effective amount of one or more compounds that include moclobemide, clorgyline, clorgyline's Near-infra-red dye Monoamine Oxidase Inhibitor (NMI), and MHI 148-clorgyline, and their salt thereof. The composition and method are particularly effective in reducing the size of glioblastomas that are temozolomide (TMZ) resistant.

  提供了一种治疗脑癌的药物组合物和方法。该方法包括向有需要的患者施用有效量的一种或多种化合物，这些化合物包括吗氯贝胺、氯吉林、氯吉林的近红染料单胺氧化酶抑制剂（NMI）和MHI 148-氯吉林，以及它们的盐。该组合物和方法对减小对替莫唑胺（TMZ）耐药的胶质母细胞瘤的体积特别有效。
• Asymmetric synthesis of l-DOPA and (R)-selegiline via, OsO4-catalyzed asymmetric dihydroxylation
  作者：Iliyas Ali Sayyed、Arumugam Sudalai

  DOI：10.1016/j.tetasy.2004.08.007

  日期：2004.10

  A simple and effective procedure for the enantioselective synthesis of two important neurotransmitter drugs, hat is, (S)-3,4-dihydroxyphenylalanine (L-DOPA) and (R)-N,alpha-dimethyl-N-2-propynylbenzeneethaneamine [(R)-selegiline], is described by employing the Sharpless asymmetric dihydroxylation (AD) as a key step to introduce chirality. (C) 2004 Elsevier Ltd. All rights reserved.
• MACGREGOR, R. R.;FOWLER, J. S.;WOLF, A. P.;HALLDIN, C.;LANGSTROM, B., J. LABELL. COMPOUNDS AND RADIOPHARM., 25,(1988) N 1, 1-9
  作者：MACGREGOR, R. R.、FOWLER, J. S.、WOLF, A. P.、HALLDIN, C.、LANGSTROM, B.

  DOI：——

  日期：——
• PHARMACEUTICAL COMPOSITION FORMULATED FOR PRE-GASTRIC ABSORPTION OF MONOAMINE OXIDASE B INHIBITORS
  申请人：Brewer Francesca Mary

  公开号：US20100227933A1

  公开（公告）日：2010-09-09

  The invention described herein provides a fast dispersing oral solid dosage form containing monoamine oxidase B inhibitor (MAO-B inhibitor) as the active ingredient, and method of treating disease therewith, such as Parkinson's disease. In one embodiment, the monoamine oxidase B inhibitor selegiline or its analogue can be the sole active ingredient in the composition administered. The dosage form composition is formulated to promote absorption through the buccal, sublingual, pharyngeal and/or esophageal mucous membrane tissue, such that at least 5% of the active ingredient is absorbed within one minute of placement in the oral cavity, as determined by a buccal absorption test. Monoamine oxidase B inhibitor compounds administered in accordance with the invention decrease the amount of undesirable metabolites associated with first pass effect of selegiline, for example, such as amphetamine and methamphetamine. The invention provides a number of other advantages over conventional orally administered tablet forms, including administration of monoamine oxidase B inhibitor compounds to patients that have difficulty swallowing.