(2R)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-4-methoxy-4-oxobutanoic acid | 339056-21-2

• 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: (2R)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-4-methoxy-4-oxobutanoic acid
• 英文别名: Fmoc-(D)Asp(Me)-OH；(2R)-β-methyl N-(9-fluorenylmethoxycarbonyl)aspartate；β-methyl N-(Fmoc)-D-aspartate；Fmoc-D-Asp(OMe)-OH；(R)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-4-methoxy-4-oxobutanoic acid；(2R)-2-(9H-fluoren-9-ylmethoxycarbonylamino)-4-methoxy-4-oxobutanoic acid
• CAS: 339056-21-2
• 化学式: C₂₀H₁₉NO₆
• 分子量: 369.374
• InChiKey: HSOKCYGOTGVDHL-QGZVFWFLSA-N

物化性质

• 沸点：
  613.7±55.0 °C(Predicted)
• 密度：
  1.322±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (2R)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-4-methoxy-4-oxobutanoic acid 在 N-甲基吗啉 、 氯甲酸异丁酯 、 甲醇 、 sodium tetrahydroborate 作用下， 以 四氢呋喃 为溶剂， 反应 2.83h， 生成 (R)-methyl 3-[N-(9-fluorenylmethoxycarbonyl)amino]-4-hydroxybutanoate
  参考文献：
  名称：

  Jamieson, Andrew G.; Boutard, Nicolas; Beauregard, Kim, Journal of the American Chemical Society, 2009, vol. 131, p. 7917 - 7927

  摘要：

  DOI：
• 作为产物：
  描述：

  甲醇 、 D-天门冬氨酸 、 9-芴甲基-N-琥珀酰亚胺基碳酸酯 在 乙酰氯 、 sodium carbonate 作用下， 以 水 、 1,4-二氧六环 为溶剂， 反应 18.0h， 生成 (2R)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-4-methoxy-4-oxobutanoic acid
  参考文献：
  名称：

  Jamieson, Andrew G.; Boutard, Nicolas; Beauregard, Kim, Journal of the American Chemical Society, 2009, vol. 131, p. 7917 - 7927

  摘要：

  DOI：

文献信息

• [EN] METHODS AND COMPOUNDS FOR THE TREATMENT OF GENETIC DISEASE<br/>[FR] PROCÉDÉS ET COMPOSÉS POUR LE TRAITEMENT D'UNE MALADIE GÉNÉTIQUE
  申请人：DESIGN THERAPEUTICS INC

  公开号：WO2021158707A1

  公开（公告）日：2021-08-12

  The present disclosure relates to compounds and methods for modulating the expression of dmpk, and treating diseases and conditions in which dmpk plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a nucleotide repeat sequence CAG or CTG; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence CAG or CTG; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.

  本公开涉及化合物和方法，用于调节dmpk的表达，并治疗dmpk发挥积极作用的疾病和病况。该化合物可以是一种转录调节分子，具有第一末端、第二末端和寡聚骨架，其中：a）第一末端包括一种DNA结合基团，能够非共价结合到核苷酸重复序列CAG或CTG；b）第二末端包括结合到调节分子的蛋白结合基团，该调节分子调节包含核苷酸重复序列CAG或CTG的基因的表达；c）寡聚骨架包括连接第一末端和第二末端的连接物。
• Solid-Phase Synthesis of Tetrahydropyridazinedione-Constrained Peptides
  作者：Chang Won Kang、Sujeewa Ranatunga、Matthew P. Sarnowski、Juan R. Del Valle

  DOI：10.1021/ol5026684

  日期：2014.10.17

  acids suitable for chemoselective incorporation into growing peptide chains. Acid-catalyzed cyclization to form the Tpd ring during cleavage affords the target peptidomimetics in good yield and purity. The scope of Tpd incorporation is demonstrated through the synthesis of constrained peptides featuring nucleophilic/electrophilic side chains and sterically encumbered α-substituted hydrazino acid residues

  报道了衍生自骨架胺化肽的四氢哒嗪-3,6-二酮 (Tpd) 肽模拟物的设计和固相合成。所描述的协议的特点是手性 α-肼酸的合成适用于化学选择性掺入不断增长的肽链。在裂解过程中酸催化环化形成 Tpd 环以良好的产率和纯度提供目标肽模拟物。Tpd 掺入的范围通过合成具有亲核/亲电侧链和空间位阻的 α-取代肼酸残基的受限肽来证明。
• HUMAN GLUCAGON-LIKE PEPTIDE-1 MIMICS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS
  申请人：Natarajan Iyer Sesha

  公开号：US20070287670A1

  公开（公告）日：2007-12-13

  The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.

  本发明提供了新型的人类胰高血糖素样肽-1 (GLP-1) 肽类模拟物，这些模拟物模仿了天然的 GLP-1 肽的生物活性，因此可用于治疗或预防与 GLP 活性相关的疾病或疾病。此外，本发明提供了新型的化学修饰肽，这些肽不仅可以刺激 II 型糖尿病患者的胰岛素分泌，还可以产生其他有益的胰岛素促进反应。这些合成的 GLP-1 模拟物肽类表现出对蛋白酶水解的稳定性增加，使它们成为口服或静脉注射治疗的理想候选药物。
• METHODS AND COMPOUNDS FOR THE TREATMENT OF GENETIC DISEASE
  申请人：Design Therapeutics, Inc.

  公开号：EP4100404A1

  公开（公告）日：2022-12-14
• Homogeneous Erythropoietin and Other Peptides and Proteins, Methods and Intermediates for Their Preparation
  申请人：Danishefsky Samuel J.

  公开号：US20100081786A1

  公开（公告）日：2010-04-01

  The present invention provides isolated homogeneous polyfunctionalized proteins (e.g., erythropoietin), isolated glycopeptides, and a method for preparing polyfunctionalized peptides and/or proteins via cysteine-free native chemical ligation. In certain embodiments, the invention provides an isolated homogeneous polyfunctionalized protein having the structure (I). In certain other embodiments, the invention provides an isolated glycopeptide having Formula (II). In certain other embodiments, the inventive method is a method for preparing a polyfunctionalized peptide comprising a peptidic backbone made up of four or more amino acids, wherein two or more non-adjacent amino acids are independently substituted with a moiety having the structure (III)-LH. wherein A and L1 are as defined herein.