D,L-N-acetyl-tryptophanamide | 10346-41-5

• 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: D,L-N-acetyl-tryptophanamide
• 英文别名: N-Acetyl-tryptophanamid；N-acetyltryptophanamide；Acetyltryptophanamid；Ac-Trp-NH2；2-acetamido-3-(1H-indol-3-yl)propanamide
• CAS: 10346-41-5
• 化学式: C₁₃H₁₅N₃O₂
• 分子量: 245.281
• InChiKey: HNGIZKAMDMBRKJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  88
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-巯基乙醇 、 D,L-N-acetyl-tryptophanamide 在 mercury(II) diacetate 作用下， 以 溶剂黄146 为溶剂， 反应 22.0h， 以38.8%的产率得到N-acetyl-L-2-<(2-hydroxyethyl)thio>tryptophanamide
  参考文献：
  名称：

  肽合成中的副反应：在乙酸水溶液中用乙酸汞（II）/ 2-巯基乙醇处理过程中色氨酸的修饰

  摘要：

  当乙酸汞（II）/ 2-巯基乙醇的水溶液 在肽合成中，使用乙酸去除乙酰氨基甲基，对Trp残基进行修饰。

  DOI：

  10.1016/0040-4039(94)88033-6
• 作为产物：
  描述：

  DL-色氨酸乙酯盐酸盐 在 氨 、 potassium carbonate 作用下， 生成 D,L-N-acetyl-tryptophanamide
  参考文献：
  名称：

  The Kinetics of the α-Chymotrypsin Catalyzed Hydrolysis of Acetyl- and Nicotinyl-L-tryptophanamide in Aqueous Solutions at 25° and pH 7.9¹

  摘要：

  DOI：

  10.1021/ja01148a040

文献信息

• Fluorescent dyes (AIDA) for solid phase and solution phase screening
  申请人：——

  公开号：US20010005752A1

  公开（公告）日：2001-06-28

  The invention relates to new fluorescent dyes of formula (I) 1 which can be used in high throughput screening both, on the solid phase as well as in homogeneous solution. The new fluorescent dyes generically referred to as AIDA chemistry is suitable for various methods of solid phase and solution phase organic chemistry for synthesis of molecules to be investigated for therapeutic use in disease states. The molecules of therapeutic interest can be synthesized as fluorescent conjugates by two methods: (a) a solid support is loaded with a cleavable linker (acid-, base-, redox- or light sensitive) to which initially the fluorescent dye is attached. The dyes possess a second functionality, which serves as attachment point for spacer elements. The spacer bears a further functional group which is used as starting point of the synthesis of the molecules to be investigated; (b) the fluorescent dye can also be introduced as end-cap in the last synthesis step of a reaction sequence. The dyes described in the invention are chemically stable under a broad range of reaction conditions usually applied in solid phase and solution phase organic chemistry. The conjugates emit fluoresence in the visible and UV-spectral range on excitation at wavelengths of their absorption. These fluorescence properties allow for multiple applications in fluorescence based processes for the identification of inhibitors of molecular interactions and for the identification of molecules which bind to target macromolecules like peptides proteins, nucleic acids, carbohydrates etc. The fluorescence detection technologies used for monitoring binding of AIDA-conjugated compounds to macromolecules include conventional macroscopic techniques (ensemble averaging) which detect changes in fluorescence intensity, anisotropy(polarization), fluorescence resonance energy transfer, fluorescence lifetime, rotational correlation time as well as one- and twodimensional single molecule spectroscopic techniques (SMS). Uses of the dye include solid phase and solution phase organic chemistry, low molecular weight compound labelling, peptide labelling, protein labelling, optical spectroscopy and fluorescence. Synthesis of functionalized dyes and of dye conjugates (on solid support and in solution) are disclosed.

  本发明涉及一种新的荧光染料，其化学式为（I）1，可用于高通量筛选，包括固相和均相溶液。这种新的荧光染料通常被称为AIDA化学，适用于各种固相和溶液相有机化学方法，用于合成用于治疗疾病状态的分子。治疗感兴趣的分子可以通过两种方法合成为荧光共轭物：（a）将可剥离连接剂（酸、碱、氧化还原或光敏）附加到固定支持上，最初将荧光染料附加到连接剂上。这些染料具有第二个功能，用作间隔元素的附着点。间隔元素带有另一个功能基团，用作待研究分子合成的起点；（b）荧光染料也可以在反应序列的最后合成步骤中作为末端盖引入。本发明中描述的染料在固相和溶液相有机化学中通常应用的广泛反应条件下具有化学稳定性。共轭物在激发其吸收波长时在可见光和紫外光谱范围内发射荧光。这些荧光特性允许在多种荧光基于过程中应用，用于鉴定分子相互作用的抑制剂以及结合到目标大分子（如肽、蛋白质、核酸、碳水化合物等）的分子的鉴定。用于监测AIDA共轭化合物与大分子结合的荧光检测技术包括传统的宏观技术（集合平均），用于检测荧光强度、各向异性（极化度）、荧光共振能量转移、荧光寿命、旋转相关时间以及一维和二维单分子光谱技术（SMS）。染料的用途包括固相和溶液相有机化学、低分子量化合物标记、肽标记、蛋白质标记、光学光谱学和荧光。本发明还公开了功能化染料和染料共轭物（在固定支持和溶液中）的合成方法。
• Macrolide antibiotics
  申请人：——

  公开号：US20040077557A1

  公开（公告）日：2004-04-22

  The present invention relates to 11,12 &ggr; lactone ketolides of formula (I) wherein R, R 1 , R 2 , R 3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

  本发明涉及公式（I）中的11,12 &ggr;内酯酮类化合物，其中R、R1、R2、R3如本文所定义的，以及其药学上可接受的盐和溶剂化物，以及它们的制备方法及在人或动物体内治疗或预防全身或局部细菌感染中的应用。
• Macrolide Antibiotics
  申请人：ALIHODZIC Sulejman

  公开号：US20060211636A1

  公开（公告）日：2006-09-21

  The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R 1 , R 2 , R 3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

  本发明涉及式(I)的11,12-γ内酯酮类化合物，其中R、R1、R2、R3如定义所述，以及其药学上可接受的盐和溶剂化物，以及其制备方法和在人或动物体内治疗或预防系统性或局部细菌感染的用途。
• PREPARATIONS STABILIZED OVER LONG TIME
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1260230A1

  公开（公告）日：2002-11-27

  A stable protein formulation containing tryptophan or a tryptophan derivative or a salt thereof as a stabilizer.

  一种含有色氨酸或色氨酸衍生物或其盐作为稳定剂的稳定蛋白质制剂。
• STABILIZED PREPARATIONS CONTAINING ANTIBODY
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1428537A1

  公开（公告）日：2004-06-16

  A stabilized antibody-containing preparation containing acetyltryptophan or an acetyltryptophan derivative or a salt thereof as a stabilizer for controlling the decrease in the biological activity of the antibody.

  一种含有乙酰色氨酸或乙酰色氨酸衍生物或其盐作为稳定剂的稳定抗体制剂，用于控制抗体生物活性的降低。

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