N-(2-methylphenyl)-L-alanine

• 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: N-(2-methylphenyl)-L-alanine
• 英文别名: 2-Methylphenyl-L-alanine；(2S)-2-(2-methylanilino)propanoic acid
• 化学式: C₁₀H₁₃NO₂
• 分子量: 179.219
• InChiKey: DLAWSMCMCKJYCA-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-碘代甲苯 、 L-丙氨酸 在 copper(l) iodide 、 2-(2-甲基-1-氧代丙烷)环己酮 、 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 以84%的产率得到N-(2-methylphenyl)-L-alanine
  参考文献：
  名称：

  使用铜（i）和β-二酮对氨基酸和肽进行室温N-芳基化†

  摘要：

  描述了一种用于两性离子氨基酸，氨基酸酯和肽的N-芳基化的温和且有效的方法。该方法提供了第一个室温下使用CuI作为催化剂，二酮作为配体，芳基碘化物作为偶联伴侣的N-芳基化氨基酸和多肽的室温合成方法。该方法同样适用于在80°C下使用相对便宜的芳基溴化物作为偶联伙伴。使用该程序，可以有效地以良好至优异的产率偶联含有反应性官能团的电子和空间上不同的芳基卤化物。

  DOI：

  10.1039/c5ob00288e

文献信息

• Process for the preparation of high purity perindopril
  申请人：Simig Guyla

  公开号：US20070197821A1

  公开（公告）日：2007-08-23

  The invention relates to 1-2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)octahydroindol-2(S)-carboxylic acid of the Formula I and the t-butylamine salt of the Formula I′ thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III (wherein R stands for lower alkyl or aryl lower alkyl). The compound of the Formula I—perindopril—is a known ACE inhibitor.

  本发明涉及公式I的1-2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)八氢吲哚-2(S)-羧酸及其不含二环己基氨基甲酸酯污染物的t-丁基胺盐的制备方法。本发明还涉及一般公式III的新中间体（其中R代表低碳基或芳基低碳基）。公式I化合物perindopril是一种已知的ACE抑制剂。
• PHENYLPHOSPHONATE FLAME RETARDANT COMPOSITIONS
  申请人：Xalter Rainer

  公开号：US20120108712A1

  公开（公告）日：2012-05-03

  The present invention relates to flame retardant polymer compositions which comprise mixtures of melamine or guanidine phenylphosphonates and mixtures with 2,2,6,6-tetraalkyl-piperidines. The mixtures are especially useful for the manufacture of flame retardant compositions based on thermoplastic polymers.

  本发明涉及阻燃聚合物组合物，其包含三聚氰胺或鸟氨酸苯基膦酸盐和2,2,6,6-四烷基哌啶的混合物。这些混合物特别适用于基于热塑性聚合物的阻燃组合物的制造。
• Sustained-release preparation
  申请人：——

  公开号：US20020058622A1

  公开（公告）日：2002-05-16

  According to a first embodiment, there is provided a sustained-release preparation comprising a water-insoluble or slightly water-soluble polyvalent metal salt of a water-soluble physiologically active substance which is not an endothelin antagonist, and a biodegradable polymer. The sustained-release preparation of the first embodiment is highly efficient in incorporating the water-soluble physiologically active substance and suppresses the initial burst of the water-soluble physiologically active substance. The sustained-release preparation of the present invention is capable of releasing the water-soluble physiologically active substance while retaining its bioactivity after administration in vivo. Furthermore, the water-soluble physiologically active substance in the sustained-release preparation is kept stable for a long period of time, with little loss of bioactivity. According to a second embodiment, there is provided a sustained-release preparation comprising an anti-endothelin substance and a biodegradable polymer. The sustained-release preparation of the present invention sustainedly releases an anti-endothelin substance, serving well in the treatment of endothelin-associated diseases.

  根据第一个实施方案，提供了一种缓释制剂，该制剂包含一种不溶于水或微溶于水的水溶性生理活性物质的多价金属盐，该生理活性物质不是内皮素拮抗剂，还包含一种可生物降解的聚合物。第一实施方案中的缓释制剂能高效地掺入水溶性生理活性物质，并抑制水溶性生理活性物质的初始迸发。本发明的缓释制剂能够释放水溶性生理活性物质，同时在体内给药后保持其生物活性。此外，本发明的缓释制剂中的水溶性生理活性物质可保持长期稳定，生物活性损失小。 根据第二个实施方案，本发明提供了一种由抗内皮素物质和生物可降解聚合物组成的缓释制剂。本发明的缓释制剂可持续释放抗内皮素物质，在治疗内皮素相关疾病中发挥良好作用。
• Non-toxic corrosion-protection pigments based on manganese
  申请人：——

  公开号：US20040011252A1

  公开（公告）日：2004-01-22

  Corrosion-inhibiting pigments based on manganese are described that contain a trivalent or tetravalent manganese/valence stabilizer complex. An inorganic or organic material is used to stabilize the trivalent or tetravalent manganese ion to form a compound that is sparingly soluble, exhibits low solubility, or is insoluble in water, depending upon the intended usage. Specific stabilizers are chosen to control the release rate of trivalent or tetravalent manganese during exposure to water and to tailor the compatibility of the powder when used as a pigment in a chosen binder system. Stabilizers may also modify the processing and handling characteristics of the formed powders. Manganese/valence stabilizer combinations are chosen based on the well-founded principles of manganese coordination chemistry. Many manganese-valence stabilizer combinations are presented that can equal the performance of conventional hexavalent chromium or tetravalent lead systems. It is emphasized that this abstract is provided to comply with the rules requiring an abstract which will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims.

  以锰为基础的缓蚀颜料含有三价或四价锰/价稳定剂复合物。一种无机或有机材料可用于稳定三价或四价锰离子，从而形成一种可少量溶解、溶解度低或不溶于水的化合物，具体取决于预期用途。选择特定的稳定剂是为了控制三价锰或四价锰在遇水时的释放率，并调整粉末在所选粘合剂体系中用作颜料时的相容性。稳定剂还可以改变成型粉末的加工和处理特性。锰/价稳定剂组合的选择是基于锰配位化学的基本原理。文中介绍了许多锰价稳定剂组合，其性能与传统的六价铬或四价铅体系相当。需要强调的是，提供本摘要是为了符合要求提供摘要的规则，以便检索者或其他读者快速确定技术公开的主题。提交本摘要的前提是，本摘要不用于解释或限制权利要求的范围或含义。
• Non-toxic corrosion-protection pigments based on rare earth elements
  申请人：——

  公开号：US20040104377A1

  公开（公告）日：2004-06-03

  A corrosion-inhibiting pigment comprising a rare earth element and a valence stabilizer combinded to form a rare earth/valence stabilizer complex. The rare earth element is selected from cerium, terbium, praseodymium, or a combination thereof, and at least one rare earth element is in the tetravalent oxidation state. An inorganic or organic material is used to stabilize the tetravalent rare earth ion to form a compound that is sparingly soluble in water. Specific stabilizers are chosen to control the release rate of tetravalent cerium, terbium, or praseodymium during exposure to water and to tailor the compatibility of the powder when used as a pigment in a chosen binder system. Stabilizers may also modify the processing and handling characteristics of the formed powders. Many rare earth-valence stabilizer combinations are presented that can equal the performance of conventional hexavalent chromium systems.

  一种缓蚀颜料，由稀土元素和价态稳定剂结合形成稀土/价态稳定剂复合物。稀土元素选自铈、铽、镨或它们的组合，至少有一种稀土元素处于四价氧化态。使用无机或有机材料来稳定四价稀土离子，以形成稀溶于水的化合物。选择特定的稳定剂是为了控制四价铈、铽或镨在遇水时的释放率，并调整粉末在所选粘合剂体系中用作颜料时的相容性。稳定剂还可以改变成型粉末的加工和处理特性。本文介绍了许多稀土-价稳定剂组合，其性能可与传统的六价铬体系媲美。