乙基L-亮氨酰甘氨酸酯 | 53375-57-8

• 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: 乙基L-亮氨酰甘氨酸酯
• 英文名称: H-Leu-Gly-OEt
• 英文别名: N-L-leucyl-glycine ethyl ester；N-L-Leucyl-glycin-aethylester；L-Leucyl=>glycin-aethylester；L-leucyl glycine ethyl ester；H-Leu-gly-oet hcl；ethyl 2-[[(2S)-2-amino-4-methylpentanoyl]amino]acetate
• CAS: 53375-57-8
• 化学式: C₁₀H₂₀N₂O₃
• 分子量: 216.28
• InChiKey: PMKXAKKWRBOEIC-QMMMGPOBSA-N

物化性质

• 沸点：
  344.1±22.0 °C(Predicted)
• 密度：
  1.042±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  81.4
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 海关编码：
  2924199090

反应信息

• 作为反应物：
  描述：

  乙基L-亮氨酰甘氨酸酯 在 palladium dihydroxide 氨 、 氢气 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 106.0h， 生成 (3S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-3-carboxamide
  参考文献：
  名称：

  β-Analogs of PLG (l-prolyl-l-leucyl-glycinamide): Ex-chiral pool syntheses and dopamine D2 receptor modulating effects

  摘要：

  Starting from (S)- and (R)-aspartic acid enantiomerically pure P-proline derivatives were synthesized. These chiral building blocks were transformed into P-analogs of the dopamine receptor modulating peptide PLG. According to dopamine receptor binding studies, significant enhancement of [H-3]pramipexole binding was observed for the isomeres 1a,b and 2a-c. The derivative Ib revealed an activity comparable to PLG. (C) 1998 Elsevier Science Ltd. Air rights reserved.

  DOI：

  10.1016/s0960-894x(98)00507-1
• 作为产物：
  描述：

  N-苄氧羰基-L-亮氨酸 在 氢溴酸 、 溶剂黄146 、 仲丁基氯甲酸酯 作用下， 生成 乙基L-亮氨酰甘氨酸酯
  参考文献：
  名称：

  Zaoral; Rudinger, Collection of Czechoslovak Chemical Communications, 1955, vol. 20, p. 1183,1185

  摘要：

  DOI：

文献信息

• Effect of solvent on the cis–trans conformational equilibrium of a proline imide bond of short model peptides in solution
  作者：Masae Sugawara、Kenji Tonan、Shun-ichi Ikawa

  DOI：10.1016/s1386-1425(00)00493-5

  日期：2001.5

  prolyl- (Boc-Leu-Pro-) were measured in mixed solvents of hexadeuterodimethylsulfoxide and deuterochloroform (CDCl3). Population ratios of cis and trans conformers with respect to the proline imide bond and chemical shifts of NH protons were obtained as a function of a CDCl3 fraction of solvent. With increasing fraction of CDCl3, the trans percentages of the Ac-Pro-imide bonds increased. On the other

  含脯氨酸的短肽的质子NMR光谱，具有N-乙酰基-脯氨酰基-（Ac-Pro-）N-叔丁氧基羰基-苯丙氨酰-脯氨酰基-（Boc-Phe-Pro-）和N-叔-在六氘代二甲基亚砜和氘代氯仿（CDCl3）的混合溶剂中测量了丁氧基羰基-亮氨酰-脯氨酰基-（Boc-Leu-Pro-）。获得相对于脯氨酸酰亚胺键的顺式和反式构象体的种群比例以及NH质子的化学位移，其是溶剂的CDCl3分数的函数。随着CDCl 3分数的增加，Ac-Pro-酰亚胺键的反式百分比增加。另一方面，Boc-Phe-Pro-的含量下降，而Boc-Leu-Pro-的含量下降趋势中等。从NH质子化学位移的溶剂依赖性变化来看，讨论了稳定Ac-Pro-的反式和Boc-Phe-Pro-的顺式的分子内氢键。对于Ac-Pro-肽，仅发现反式与7、10和13元氢键环兼容，这与普通的二级结构，γ-和β-转角以及α相似-螺旋。对于Boc-Phe-Pro-R的顺式形式（R
• PEPTIDE SYNTHESIS BY USING<i>N</i>-ACYLPHOSPHORAMIDITES
  作者：Wataru Kawanobe、Kazuo Yamaguchi、Seiichi Nakahama、Noboru Yamazaki

  DOI：10.1246/cl.1982.825

  日期：1982.6.5

  New trivalent phosphorus compounds, N-acetyl-N-methylphosphoramidites were prepared readily in good yield by the reaction of phosphorous chlorides and N-methylacetamide. By using the phosphoramidites as condensing agents, Young’s peptide and prolyl-leucyl-glycinamede(MSH-RIF) were synthesized without racemization in high yields under mild conditions.

  新型三价磷化合物N-乙酰基-N-甲基磷酰胺以良好的产率通过磷氯化物与N-甲基乙酰胺的反应制备而成。利用这些磷酰胺作为缩合剂，Young的肽和脯氨酸-亮氨酸-甘氨酸酰胺（MSH-RIF）在温和条件下高产率合成且未发生消旋现象。
• Synthesis and Circular Dichroism Spectra of Sperm Whale Myoglobin-(57-96)-Tetracontapeptide.
  作者：Chikao Hashimoto、Ichiro Muramatsu

  DOI：10.1246/bcsj.66.181

  日期：——

  A protected sperm whale myoglobin-(57—96)-tetracontapeptide (29) was synthesized by successive condensations of three fragments, Boc–(70 —76)–OH, Boc–(62—69)–OH, and Boc–(57— 61)–OH, to a partially protected eicosapeptide ester, H–(77—96)– OBzl. After removal of the protecting groups of 29, the crude product was purified with reversed-phase high-performance liquid chromatography to yield sperm whale myoglobin-(57—96)-tetracontapeptide (30). The circular dichroism spectra showed that this peptide was in a random conformation in 0.10 M phosphate buffer (pH 6.50) and in a 69% α-helix conformation in 60% 2,2,2-trifluoroethanol–0.10 M phosphate buffer (pH 6.50).

  通过连续缩合三个片段 Boc–(70 —76)–OH、Boc–(62–69)–OH 和 Boc–(57) 合成了受保护的抹香鲸肌红蛋白-(57—96)-十碳肽 (29) — 61)–OH，部分保护的二十肽酯，H–(77–96)– OBzl。去除29的保护基后，用反相高效液相色谱纯化粗产物，得到抹香鲸肌红蛋白-(57—96)-四十二肽(30)。圆二色光谱显示该肽在 0.10 M 磷酸盐缓冲液 (pH 6.50) 中呈随机构象，在 60% 2,2,2-三氟乙醇–0.10 M 磷酸盐缓冲液 (pH 6.50) 中呈 69% α-螺旋构象。
• [EN] NOVEL ESTERS OF (ACYLOXYMETHYL)ACRYLAMIDE, A PHARMACEUTICAL COMPOSITION CONTAINING THEM, AND THEIR USE AS INHIBITORS OF THE THIOREDOXIN - THIOREDOXIN REDUCTASE SYSTEM<br/>[FR] NOUVEAUX ESTERS D'(ACYLOXYMÉTHYL)ACRYLAMIDE, COMPOSITION PHARMACEUTIQUE LES CONTENANT, ET LEUR UTILISATION EN TANT QU'INHIBITEURS DU SYSTÈME DE THIORÉDOXINE/THIORÉDOXINE RÉDUCTASE
  申请人：INST CHEMII ORGANICZNEJ POLSKIEJ AKADEMII NAUK

  公开号：WO2012050465A1

  公开（公告）日：2012-04-19

  The subject of the present invention are novel esters of (acyloxymethyl)acrylamide, a pharmaceutical composition containing them and their use in the production of drugs for the prophylaxis or treatment of oncogenic diseases and diseases connected with increased cell proliferation.

  本发明的主题是新的（酰氧甲基）丙烯酰胺酯，其中包含它们的制药组合物以及它们在生产用于预防或治疗肿瘤性疾病和与细胞增殖增加有关的疾病的药物中的应用。
• Human interferon-related peptides, antigens, antibodies and process for
  申请人：Otsuka Pharmaceutical Co., Ltd.

  公开号：US04474754A1

  公开（公告）日：1984-10-02

  Human interferons related peptides and derivatives thereof, antigens, antibodies prepared therefrom, immobilized antibodies to be used for affinity chromatography, and novel method for assaying human interferons by using said affinity chromatography.

  人类干扰素相关肽及其衍生物，抗原，由此制备的抗体，用于亲和层析的固定化抗体以及利用该亲和层析的新方法来检测人类干扰素。