(2R)-2-[(phenylsulfonyl)amino]propanoic acid | 29268-17-5

• 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-[(phenylsulfonyl)amino]propanoic acid
• 英文别名: (R)-(+)-N-(Benzolsulfonyl)-alanin；N-benzenesulfonyl-D-alanine；N-Benzolsulfonyl-D-alanin；(2R)-2-benzenesulfonamidopropanoic acid；(2R)-2-(benzenesulfonamido)propanoic acid
• CAS: 29268-17-5
• 化学式: C₉H₁₁NO₄S
• mdl: MFCD20502029
• 分子量: 229.257
• InChiKey: KHLXTMZRKBVYST-SSDOTTSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.222
• 拓扑面积：
  91.8
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-氨基-5-苯基-1,3,4-噻二唑 、 (2R)-2-[(phenylsulfonyl)amino]propanoic acid 在 N-羟基丁二酰亚胺 、 N,N'-二环己基碳二亚胺 作用下， 以 1,4-二氧六环 为溶剂， 反应 48.0h， 以25.8%的产率得到(2R)-N-[5-phenyl-1,3,4-thiadiazol-2-yl]-2-[(phenylsulfonyl)amino]propanamide
  参考文献：
  名称：

  Synthesis of 1,3,4-thiadiazole derivatives as aminopeptidase N inhibitors

  摘要：

  氨肽酶N（APN）是一种锌依赖性外肽酶，在转移性肿瘤的侵袭过程中起重要作用。在本研究中，我们报道了1,3,4-噻二唑骨架化合物的合成及其体外酶抑制活性测定。这些新化合物对APN表现出强效的抑制活性，IC50值在微摩尔范围内。

  DOI：

  10.1691/ph.2009.8630
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 L-(-)-去甲伪麻黄碱 、 水 作用下， 生成 (2R)-2-[(phenylsulfonyl)amino]propanoic acid
  参考文献：
  名称：

  Gibson; Levin, Journal of the Chemical Society, 1929, p. 2757

  摘要：

  DOI：

文献信息

• Thiadiazines and their use as inhibitors of metalloproteinases
  申请人：Tschesche, Harald

  公开号：EP1191024A1

  公开（公告）日：2002-03-27

  The present invention provides novel thiadiazines represented by formula (I) which are useful as inhibitors of metalloproteinases. Also disclosed are pharmaceutical compositions and methods of treating disorders associated with increased activity of metalloproteinases using these compounds or the pharmaceutical compositions containing them.

  本发明提供了一种新型的噻二唑类化合物，其化学式表示为（I），这些化合物可用作金属蛋白酶的抑制剂。还公开了使用这些化合物或含有它们的药物组合物治疗与金属蛋白酶活性增加相关的疾病的方法和药物组合物。
• [EN] AMINOQUINOLINE DERIVATIVES AS ANTIVIRAL AGENTS<br/>[FR] DÉRIVÉS D'AMINOQUINOLÉINE COMME AGENTS ANTIVIRAUX
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2012037108A1

  公开（公告）日：2012-03-22

  Provided are compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).

  提供的是式(I)和式(II)的化合物及其药用盐，它们的药物组合物，它们的制备方法，以及它们用于治疗由黄病毒科病毒介导的病毒感染，如丙型肝炎病毒（HCV）。
• [EN] PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED 3-AMINOPIPERIDINE<br/>[FR] PROCÉDÉ DE PRÉPARATION D'UNE 3-AMINOPIPÉRIDINE ENRICHIE EN ÉNANTIOMÈRES
  申请人：REUTER CHEMISCHE APPBAU KG

  公开号：WO2014128139A1

  公开（公告）日：2014-08-28

  The present invention relates to a process for the preparation of enantiomerically enriched 3-aminopiperidine, and in particular of its R-enantiomer (R)-3-aminopiperidine. The invention also relates to an enantiomerically enriched intermediate of said process and to specific acid-addition salts of 3-aminopiperidine (hereinafter also APIP) that are useful for obtaining a single enantiomer of APIP, and to crystalline (R)-3-aminopiperidine-dihydrochloride-monohydrateand crystalline (S)-3-aminopiperidine-dihydrochloride-monohydrate.

  本发明涉及一种制备对映体富集的3-氨基哌啶的方法，特别是其R-对映体（R）-3-氨基哌啶。该发明还涉及该过程的对映体富集中间体，以及对3-氨基哌啶（以下简称APIP）的特定酸加盐，用于获得APIP的单一对映体，并且涉及结晶的（R）-3-氨基哌啶二盐酸盐一水合物和结晶的（S）-3-氨基哌啶二盐酸盐一水合物。
• PARAKERATOSIS INHIBITOR, PORE-SHRINKING AGENT OR AGENT FOR PREVENTING/AMELIORATING ROUGH SKIN AND EXTERNAL COMPOSITION FOR SKIN
  申请人：Shiseido Company, Limited

  公开号：EP1884230A1

  公开（公告）日：2008-02-06

  The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin -inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and to further provide an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor agent, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof. The external composition for skin comprises the one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.

  该发明提供了一种具有角化不全抑制、收缩毛孔或防止/改善粗糙皮肤功能的抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂，不会引起感觉刺激等安全问题，非常安全，并进一步提供了一种外用皮肤组合物，其中添加了具有上述功能的化合物。角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂包括从α-氨基酸衍生物和其盐组成的群中选择的一种、两种或更多化合物。外用皮肤组合物包括从α-氨基酸衍生物和其盐组成的群中选择的一种、两种或更多化合物，作为上述角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂。
• Parakeratosis inhibitor, pore-shrinking agent,or rough skin preventing/ameliorating agent, and external composition for skin
  申请人：Kaminuma Mikiko

  公开号：US20090215893A1

  公开（公告）日：2009-08-27

  The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin-inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and to further provide an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor agent, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof. The external composition for skin comprises the one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.

  本发明提供了一种角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂，具有角化不全抑制、毛孔收缩或防止/减轻粗糙皮肤等功能，不会引起感觉刺激等安全问题，非常安全，进一步提供了一种添加了具有上述功能的化合物的皮肤外用组合物。该角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂包含从α-氨基酸衍生物和其盐的组中选择的一种、两种或更多化合物。该皮肤外用组合物包含从α-氨基酸衍生物和其盐的组中选择的一种、两种或更多化合物，作为上述角化不全抑制剂、收缩毛孔剂或防止/改善粗糙皮肤剂。