4-氨基-L-苯丙氨酸甲酯 | 105052-56-0

• 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
• 中文名称: 4-氨基-L-苯丙氨酸甲酯
• 英文名称: H-Phe(4NH2)-OMe
• 英文别名: methy14-amino-L-phenylalaninate；methyl 4-amino-L-phenylalaninate；methyl (S)-2-amino-3-(4-aminophenyl)propanoate；4-amino-L-phenylalanine methyl ester；methyl (2S)-2-amino-3-(4-aminophenyl)propanoate
• CAS: 105052-56-0
• 化学式: C₁₀H₁₄N₂O₂
• 分子量: 194.233
• InChiKey: VWHHEDIHZWZRTF-VIFPVBQESA-N

物化性质

• 沸点：
  331.1±27.0 °C(Predicted)
• 密度：
  1.176±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  78.3
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-氨基-L-苯丙氨酸甲酯 在 叠氮阴离子 、 氢气 、 Nitrite 作用下， 以 水 为溶剂， 生成 H-Phe(4N3)-OMe
  参考文献：
  名称：

  血管紧张素II生理生化合成法

  摘要：

  具有延长的可裂解臂的生物素化探针的合成，用于血管紧张素II受体纯化

  DOI：

  10.1002/hlca.19890720409
• 作为产物：
  描述：

  (S)-4-硝基苯基丙氨酸甲酯盐酸盐 在 palladium on activated charcoal 、 氢气 作用下， 以 甲醇 为溶剂， 反应 16.0h， 以100%的产率得到4-氨基-L-苯丙氨酸甲酯
  参考文献：
  名称：

  Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ (PPARγ)

  摘要：

  Photopharmacology aims at the optical control of protein activity using synthetic photoswitches. This approach has been recently expanded to nuclear hormone receptors with the introduction of "photohormones" for the retinoic acid receptor, farnesoid X receptor, and estrogen receptor. Herein, we report the development and profiling of photoswitchable agonists for peroxisome proliferator-activated receptor gamma (PPAR gamma). Based on known PPAR gamma ligands (MDG548, GW1929, and rosiglitazone), we have designed and synthesized azobenzene derivatives, termed AzoGW1929 and AzoRosi, which were confirmed to be active in cell-based assays. Subsequent computer-aided optimization of AzoRosi resulted in the photohormone AzoRosi-4, which bound and activated PPAR gamma preferentially in its light-activated cis-configuration.

  DOI：

  10.1021/acs.jmedchem.0c00654

文献信息

• CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
  申请人：PFIZER INC.

  公开号：US20130129753A1

  公开（公告）日：2013-05-23

  The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

  本发明涉及细胞毒性五肽，其抗体药物偶联物，以及使用它们治疗癌症的方法。
• A Method for the Selective Protection of Aromatic Amines in the Presence of Aliphatic Amines
  作者：Boulos Zacharie、Valérie Perron、Shaun Abbott、Nancie Moreau、Devin Lee、Christopher Penney

  DOI：10.1055/s-0028-1083290

  日期：2009.1

  aromatic amines in the presence of aliphatic amines. The method is general for the preparation of mono-N-Boc, -N-Cbz, -N-Fmoc or -N-Alloc aromatic amines in high yield without affecting the aliphatic amines. This approach is applicable to substituted (aminoalkyl)aniline compounds with different functionalities and was employed to supply gram quantities of the protected aniline product. amines - carbamates

  已经开发了一种简单有效的方法，用于在脂肪胺存在下对芳香胺进行区域选择性保护。该方法是一般为单-的制备Ñ -Boc， - Ñ -Cbz， - ñ -Fmoc或- ñ以高收率-alloc芳香胺而不影响脂族胺。该方法适用于具有不同官能度的取代的（氨基烷基）苯胺化合物，并用于提供克量的受保护的苯胺产品。 胺-氨基甲酸酯-保护基-质子化-区域选择性
• Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
  申请人：Pierau Sabine

  公开号：US20060046978A1

  公开（公告）日：2006-03-02

  This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.

  该发明涉及新型化合物，含有这些化合物的组合物，这些化合物抑制二肽基肽酶（特别是DPP-IV）和神经肽酶（NEP，中性内肽酶）以及二肽基肽酶（特别是DPP-IV）和血管紧张素转化酶（ACE）和/或二肽基肽酶（特别是DPP-IV）和血管肽酶（特别是ACE和NEP）。这些化合物及其药物组合物对于治疗和预防2型糖尿病是有用的。
• Polypeptide and protein derivatives and process for their preparation
  申请人：——

  公开号：US20040081660A1

  公开（公告）日：2004-04-29

  Protein and polypeptid derivatives and th ir salts are claimed characteriz d in that a prot in or polypeptide is conjugated via an int rmediat grouping containing at least one radical of the formula —C(R)═N— (or —N═C(R)—) or —CH(R)—NH— (or —NH—CH(R)—), wherein R is hydrogen or a hydrocarbon residue which may be substituted, with the same or a different protein or polypeptide, with a reporter group or a cytotoxic agent as well as a process for their preparation and the novel intermediates therefor.

  本发明涉及蛋白质和多肽衍生物及其盐，其特征在于通过至少含有一个公式为—C（R）═N—（或—N═C（R）—）或—CH（R）—NH—（或—NH—CH（R）—）的中间基团与相同或不同的蛋白质或多肽结合，以及将报告基团或细胞毒性剂与其替代的氢或可被替代的碳氢残基的蛋白质或多肽结合的方法和新的中间体。
• P2'-modified hydroxamic acid collagenase inhibitors
  申请人：British Bio-Technology Limited

  公开号：US05412145A1

  公开（公告）日：1995-05-02

  Compounds of general formula I: ##STR1## Wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are variables. These compounds have collagenase inhibition activity and are useful in the management of disease involving collagen degradation. Its uses include rheumatoide arthritis, corneal ulceration, osteoporosis, periodontitis, gingivitis and tumor invasion.

  通式I的化合物：##STR1## 其中：R.sup.1，R.sup.2，R.sup.3，R.sup.4，R.sup.5和R.sup.6是变量。这些化合物具有胶原酶抑制活性，并可用于管理涉及胶原降解的疾病。其用途包括类风湿性关节炎，角膜溃疡，骨质疏松症，牙周炎，龈炎和肿瘤侵袭。