(R)-2-amino-N,4-dimethylpentanamide hydrochloride | 108131-54-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (R)-2-amino-N,4-dimethylpentanamide hydrochloride
• 英文别名: (2R)-2-amino-N,4-dimethylpentanamide;hydrochloride
• CAS: 108131-54-0
• 化学式: C₇H₁₆N₂O*ClH
• 分子量: 180.678
• InChiKey: RRZJUBLBYSGTOZ-FYZOBXCZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.53
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  55.1
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (R)-2-amino-N,4-dimethylpentanamide hydrochloride 、 2-[(2-Methylpropan-2-yl)oxycarbonylamino]-2-prop-2-ynylpent-4-ynoic acid 在 N-甲基吗啉 、 1-羟基苯并三唑 作用下， 以 四氢呋喃 为溶剂， 生成 [1-((R)-3-Methyl-1-methylcarbamoyl-butylcarbamoyl)-1-prop-2-ynyl-but-3-ynyl]-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Constrained phenylalanyl peptides via a [2+2+2]-cycloaddition strategy

  摘要：

  描述了一种可能对肽模拟和组合化学应用有价值的肽修饰，涉及[2+2+2]环加成反应，从而生成具有构象约束的苯丙氨酸肽。

  DOI：

  10.1039/b005605g

文献信息

• [EN] METHODS OF TREATING ALZHEIMER'S DISEASE USING ARYL ALKANOIC ACID AMIDES<br/>[FR] METHODES DE TRAITEMENT DE LA MALADIE D'ALZHEIMER PAR DES AMIDES D'ACIDE ARYL ALCANOIQUE
  申请人：ELAN PHARM INC

  公开号：WO2003103653A1

  公开（公告）日：2003-12-18

  Disclosed are methods for treating Alzheimer’s disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula 1 (1) wherein the variables R1-R8 and X are defined herein.

  揭示了一种治疗阿尔茨海默病和其他疾病，和/或抑制β-分泌酶，和/或通过使用式1（1）中定义的化合物在哺乳动物体内抑制Aβ肽的沉积的方法。其中变量R1-R8和X在此处定义。
• [EN] PYRIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE PYRIDINES
  申请人：HOFFMANN LA ROCHE

  公开号：WO2018234284A1

  公开（公告）日：2018-12-27

  The invention relates to compound of formula (I) wherein R1 to R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

  本发明涉及式(I)的化合物，其中R1至R3如描述和权利要求中所定义。式(I)的化合物可用作药物。
• Pyridine derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US11117903B2

  公开（公告）日：2021-09-14

  The invention relates to compound of formula (I) wherein R1 to R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

  本发明涉及式 (I) 的化合物 其中 R1 至 R3 如说明书和权利要求书中所定义。式（I）化合物可用作药物。
• Synthesis and Anticonvulsant Activity of a New Class of 2-[(Arylalkyl)amino]alkanamide Derivatives
  作者：Paolo Pevarello、Alberto Bonsignori、Philippe Dostert、Franco Heidempergher、Vittorio Pinciroli、Maristella Colombo、Robert A. McArthur、Patricia Salvati、Claes Post、Ruggero G. Fariello、Mario Varasi

  DOI：10.1021/jm970599m

  日期：1998.2.1

  Although most epilepsies are adequately treated by conventional antiepileptic therapy, there remains an unfulfilled need for safer and more effective anticonvulsant agents. Starting from milacemide, a weak anticonvulsant, and trying to elucidate its mechanism of action, we discovered a structurally novel class of potent and preclinically safe anticonvulsants. Here we report the structure-activity relationship (SAR) study within this series of compounds. Different parts of the structural lead 2-[[4-(3-chlorobenzoxy)benzyl]amino] acetamide (6) were thus varied (Figure 1), and many potent anticonvulsants were found. As an outcome of this study, 57 ((S)-2-[[4-(3-fluorobenzoxy)benzyl]amino]propanamide methanesulfonate, PNU-151774E) emerged as a promising candidate for further development for its potent anticonvulsant activity and outstanding therapeutic indexes (TIs) in different animal tests.
• PYRIDINE DERIVATIVES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3642200A1

  公开（公告）日：2020-04-29