2-(萘-2-基氨基)乙酸 | 89504-69-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: 2-(萘-2-基氨基)乙酸
• 英文名称: L-(2-Naphthyl)glycine
• 英文别名: N-(2-naphthyl)aminoacetic acid；2-naphthylglycine；N-[2]naphthyl-glycine；β-Naphthylaminoessigsaeure；N-[2]Naphthyl-glycin；N-β-Naphthyl-glycin；Glycine, N-2-naphthalenyl-；2-(naphthalen-2-ylamino)acetic acid
• CAS: 89504-69-8
• 化学式: C₁₂H₁₁NO₂
• 分子量: 201.225
• InChiKey: SEABHMYCRYLVKD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(萘-2-基氨基)乙酸 生成 1,4-di-naphthalen-2-yl-piperazine-2,5-dione
  参考文献：
  名称：

  Bischoff; Hausdoerfer, Chemische Berichte, 1890, vol. 23, p. 1998

  摘要：

  DOI：
• 作为产物：
  描述：

  ethyl naphthalen-2-ylglycinate 在 水 、 sodium hydroxide 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 生成 2-(萘-2-基氨基)乙酸
  参考文献：
  名称：

  通过光诱导脱芳构化构建桥联苯并氮杂卓

  摘要：

  开发了一种温和有效的方案，通过光催化脱芳构化将简单的芳香族底物转化为增值且结构复杂的桥联苯并氮杂卓。可通过碱促进或光诱导的分子内氢氨化的操作来提供可切换的非对映选择性。

  DOI：

  10.1002/anie.202314304

文献信息

• PROCESS FOR SYNTHESIS OF SYN AZIDO EPOXIDE AND ITS USE AS INTERMEDIATE FOR THE SYNTHESIS OF AMPRENAVIR & SAQUINAVIR
  申请人：Council of Scientific & Industrial Research

  公开号：US20150011782A1

  公开（公告）日：2015-01-08

  Disclosed herein is a novel route of synthesis of syn azide epoxide of formula 5, which is used as a common intermediate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt-catalyzed hydrolytic kinetic resolution of racemic anti-(2SR,3SR)-3-azido-4-phenyl-1,2-epoxybutane (azido-epoxide).

  本文披露了一种合成公式5的syn叠氮环氧化物的新路线，该化合物被用作HIV蛋白酶抑制剂的不对称合成的常见中间体，如Amprenavir、Fosamprenavir、Saquinavir以及通过钴催化的拆分手性反式-(2SR,3SR)-3-叠氮-4-苯基-1,2-环氧丁烷(叠氮环氧化物)合成Darunavir和Palinavir。
• [EN] SMALL LIPOPEPTIDOMIMETIC INHIBITORS OF GHRELIN O-ACYL TRANSFERASE<br/>[FR] PETITS INHIBITEURS LIPOPEPTIDOMIMÉTIQUES DE LA GHRÉLINE O-ACYL TRANSFÉRASE
  申请人：UNIV CALIFORNIA

  公开号：WO2016044467A1

  公开（公告）日：2016-03-24

  Compositions and methods are disclosed that relate to small molecule lipopeptidomimetic inhibitors of mammalian ghrelin O-acyl transferase (GOAT). Compounds of general Formula (I) and substructures thereof, i.e., Formulae (II), (IIa), (IIa1), (IIa2), (IIb), (IIb1), (IIb2), (IIc) and (III), are shown to exhibit potent inhibition of the octanoylation of ghrelin peptide, where the resulting non-octanoylated (des-acyl) form of ghrelin lacks GHSr ligand activity that is associated with weight gain and insulin resistance. These and related embodiments will find uses for treating subjects known to have, or suspected of being at risk for having, a condition that would benefit from a decreased level of acylated ghrelin peptide, such as type II diabetes, impaired glucose tolerance, insulin resistance, Prader-Willi syndrome (PWS) and obesity.

  公开了与哺乳动物生长激素释放肽O-酰基转移酶（GOAT）的小分子脂肽类似物抑制剂有关的组合物和方法。通式（I）及其亚结构，即，通式（II）、（IIa）、（IIa1）、（IIa2）、（IIb）、（IIb1）、（IIb2）、（IIc）和（III）的化合物显示出对生长激素释放肽的辛酰化反应的强大抑制作用，其中产生的非辛酰化（脱酰基）形式的生长激素释放肽缺乏与体重增加和胰岛素抵抗相关的GHSr配体活性。这些和相关实施例可用于治疗已知或怀疑有患有可能从降低酰化生长激素释放肽水平中受益的病症的患者，例如II型糖尿病、葡萄糖耐量受损、胰岛素抵抗、普拉德-威利综合症（PWS）和肥胖。
• Fas LIGAND SOLUBILIZATION INHIBITOR
  申请人：KANEBO LTD.

  公开号：EP0848957A1

  公开（公告）日：1998-06-24

  A Fas ligand solubilization inhibitor which comprises, as the active ingredient, a compound of the generic formula (I) having a matrix metalloproteinase inhibitory activity or its pharmaceutically acceptable salt. The drug is useful in the prevention or treatment of diseases caused by solubilized Fas ligand, such as hepatitis, GVHD, AIDS, autoimmune diseases, etc.

  一种Fas配体溶解抑制剂，其活性成分为具有基本结构式（I）的化合物，具有基质金属蛋白酶抑制活性或其药用盐。该药物可用于预防或治疗由溶解的Fas配体引起的疾病，如肝炎、移植物抗宿主病、艾滋病、自身免疫疾病等。
• Naphthylglycyl cephalosporin derivatives
  申请人：Eli Lilly and Company

  公开号：US04490370A1

  公开（公告）日：1984-12-25

  Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and are particularly useful as oral treatments for upper respiratory infections.

  Naphthylglycyl和tetrahydronaphthylglycyl头孢菌素是强效的抗菌剂，特别适用于口服治疗上呼吸道感染。
• Optically active bisoxazoline compounds, process for production of the same and use thereof
  申请人：Itagaki Makoto

  公开号：US20060149077A1

  公开（公告）日：2006-07-06

  Optically active bisoxazoline compounds represented by the general formula (1), a process for producing the compounds, and a process for producing cyclopropanecarboxylic esters by using the same: wherein R 1 and R 2 are the same and each represents C 1-6 alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted phenyl or R 1 and R 2 are bonded each other together with the carbon atom of oxazoline ring to which they are bonded to form a ring; R 3 is substituted or unsubstituted naphthyl; R 4 and R 5 are the same and each represent hydrogen or C 1-6 alkyl, or R 4 and R 5 are bonded each other together with the carbon atom to which they are bonded to form a cycloalkyl ring having 3 to 6 carbon atoms; and * represents an asymmetric center.

  光学活性的双噁唑啉化合物由通式（1）表示，制备该化合物的方法以及使用该化合物制备环丙烷羧酸酯的方法： 其中，R1和R2相同，分别表示C1-6烷基，取代或未取代的芳基烷基或取代或未取代的苯基，或者R1和R2相互结合形成环，与它们所连接的噁唑环的碳原子相连；R3是取代或未取代的萘基；R4和R5相同，分别表示氢或C1-6烷基，或者R4和R5相互结合形成有3至6个碳原子的环状烷基环；*表示一个不对称中心。