Fmoc-D-色氨酸 | 144701-22-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 中文名称: Fmoc-D-色氨酸
• 中文别名: FMOC-DL-色氨酸
• 英文名称: (5r)-2-(((9H-fluoren-9-yl)methoxy)carbonylamino)-3-(1H-indol-3-yl)propanoic acid
• 英文别名: 2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3-(1H-indol-3-yl)propanoic acid；N-fmoc-2-amino-3-(1H-indol-3-yl)-propionic acid；N-fluoren-9-ylmethoxycarbonyl-tryptophan；Fmoc-l-tryptophan；Fmoc-Trp- OH；Fmoc-Trp；2-(((9H-Fluoren-9-yl)methoxy)carbonylamino)-3-(1H-indol-3-yl)propanoic acid；2-(9H-fluoren-9-ylmethoxycarbonylamino)-3-(1H-indol-3-yl)propanoic acid
• CAS: 144701-22-4
• 化学式: C₂₆H₂₂N₂O₄
• 分子量: 426.472
• InChiKey: MGHMWKZOLAAOTD-UHFFFAOYSA-N

物化性质

• 沸点：
  711.9±60.0 °C(Predicted)
• 密度：
  1.350±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  91.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Fmoc-D-色氨酸 在 吡啶 、 三聚氟氰 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 [1-Fluorocarbonyl-2-(1H-indol-3-yl)-ethyl]-carbamic acid 9H-fluoren-9-ylmethyl ester
  参考文献：
  名称：

  Efficient Loading of Sulfonamide Safety-Catch Linkers by Fmoc Amino Acid Fluorides

  摘要：

  [GRAPHICS]Fmoc-protected amino acid fluorides were found to be excellent reagents for the acylation of sulfonamide safety-catch linkers (SCL) suitable for the subsequent preparation of peptide C-terminal thioesters. High loadings were obtained on different types of resins with low levels of epimerization.

  DOI：

  10.1021/ol0256320
• 作为产物：
  描述：

  氯甲酸-9-芴基甲酯 、 DL-色氨酸 生成 Fmoc-D-色氨酸
  参考文献：
  名称：

  ALLENMARK, S.;ANDERSSON, S., CHROMATOGRAPHIA, 31,(1991) N-10, C. 429-433

  摘要：

  DOI：

文献信息

• Novel chiral stationary phases based on 3,5‐dimethyl phenylcarbamoylated β‐cyclodextrin combining cinchona alkaloid moiety
  作者：Lunan Zhu、Junchen Zhu、Xiaotong Sun、Yaling Wu、Huiying Wang、Lingping Cheng、Jiawei Shen、Yanxiong Ke

  DOI：10.1002/chir.23237

  日期：2020.8

  Novel chiral selectors based on 3,5‐dimethyl phenylcarbamoylated β‐cyclodextrin connecting quinine (QN) or quinidine (QD) moiety were synthesized and immobilized on silica gel. Their chromatographic performances were investigated by comparing to the 3,5‐dimethyl phenylcarbamoylated β‐cyclodextrin (β‐CD) chiral stationary phase (CSP) and 9‐O‐(tert‐butylcarbamoyl)‐QN‐based CSP (QN‐AX). Fmoc‐protected

  合成了基于3,5-二甲基苯基氨基甲酰基化的β-环糊精连接奎宁（QN）或奎尼丁（QD）部分的新型手性选择剂，并将其固定在硅胶上。通过与3,5-二甲基苯基氨基甲酰基化的β-环糊精（β-CD）手性固定相（CSP）和9- O-（叔）进行比较，研究了它们的色谱性能。-丁基氨基甲酰基）-基于QN的CSP（QN-AX）。在CSP上评估了Fmoc保护的氨基酸，手性药物Cloprostenol（已成功用于兽医学）和中性手性分析物，结果表明，这种新型CSP既具有CD基CSP的对映体分离能力，又具有QN /与基于β-CD的CSP或基于QN / QD的CSP相比，基于QD的CSP具有更广泛的应用范围。发现QN / QD部分在Fmoc-氨基酸的整个对映体分离过程中起主导作用，并伴随有β-CD部分的协同作用，从而导致基于β-CD-QN的CSP和β的不同对映体分离基于CD-QD的CSP。此外，
• Modified aminoacids, pharmaceuticals containing these compounds and method for their production
  申请人：Dr. Karl Thomae GmbH

  公开号：US06344449B1

  公开（公告）日：2002-02-05

  The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.

  本发明涉及一般式的改性氨基酸 其中 A、Z、X、n、m、R、R2、R3、R4和R11的定义如权利要求1至5中所述，它们的互变异构体、对映异构体、立体异构体、它们的混合物及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，含有这些化合物的药物组合物，其用途以及制备它们的过程，以及它们在抗体的生产和纯化中的用途以及在RIA和ELISA测定中作为标记化合物以及在神经递质研究中作为诊断或分析辅助工具的用途。
• Solid and solution phase combinatorial synthesis of ureas
  作者：JoséW. Nieuwenhuijzen、Paolo G.M. Conti、Harry C.J. Ottenheijm、Joannes T.M. Linders

  DOI：10.1016/s0040-4039(98)01708-0

  日期：1998.10

  An efficient parallel synthesis of ureas based on amino acids is described, both in solution and on solid phase. 1,1′-Carbonylbisbenzotriazole 2 is used as the coupling reagent. The ureas 5 and 10 were obtained in high yield (80–100%) and purity (71–97%).

  描述了在溶液和固相中基于氨基酸的尿素的有效平行合成。1,1'-羰基双苯并三唑2被用作偶联剂。获得的尿素5和10的产率高（80-100％），纯度高（71-97％）。
• Pharmaceutically active sulfanilide derivatives
  申请人：——

  公开号：US20040072816A1

  公开（公告）日：2004-04-15

  The present invention relates to sulfanilide derivatives of formula (I), in which R 1 and R 2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin, including preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. The present invention is furthermore related to novel sulfanilide derivatives as well as to methods of their preparation.

  本发明涉及式(I)的磺胺基苯酰胺衍生物，其中R1和R2是可选择取代的芳基和杂环芳基基团，其他变量如权利要求中所定义，用作药用活性化合物，以及含有这种磺胺基苯酰胺衍生物的药物配方。所述衍生物在治疗和/或预防早产、早产、痛经、抗利尿素分泌不当、充血性心力衰竭、动脉高血压、肝硬化、肾病综合征和眼压增高方面具有用途。具体而言，本发明涉及显示对催产素和/或抗利尿素受体具有显著调节作用，特别是拮抗活性的磺胺基苯酰胺衍生物。更具体地说，所述化合物在治疗和/或预防由催产素和/或抗利尿素介导的疾病状态方面具有用途，包括早产、早产、痛经、抗利尿素分泌不当、充血性心力衰竭、动脉高血压、肝硬化、肾病综合征和眼压增高。本发明还涉及新型磺胺基苯酰胺衍生物以及其制备方法。
• NON-NUCLEOSIDE ANTI-HEPACIVIRUS AGENTS AND USES THEREOF
  申请人：Boyd A. Vincent

  公开号：US20070021434A1

  公开（公告）日：2007-01-25

  The present dislcosure provides amide-based, non-nucleoside compounds having antiviral activity against Hepacivirus, such as hepatitis C virus (HCV), methods and intermediates for synthesizing such compounds, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of viral infections. The present dislcosure also provides methods for identifying amide-based, non-nucleoside compounds having antiviral activity.

  本公开提供了基于酰胺的非核苷类化合物，具有抗Hepacivirus活性，例如丙型肝炎病毒（HCV），合成这类化合物的方法和中间体，以及在各种情境中使用这些化合物的方法，包括在治疗和预防病毒感染中的应用。本公开还提供了识别具有抗病毒活性的基于酰胺的非核苷类化合物的方法。