D-p-hydroxyphenylglycine amide | 143164-48-1

• 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: D-p-hydroxyphenylglycine amide
• 英文别名: p-hydroxyphenylglycine amide；4-hydroxyphenyl-glycinamide；N-(4-hydroxy-phenyl)-glycine amide；Amid aus 4-Oxy-anilinoessigsaeure；N-(4-Hydroxy-phenyl)-glycin-amid；Amid aus N-(4-Oxy-phenyl)-glycin；2-(4-hydroxyanilino)acetamide
• CAS: 143164-48-1；143235-10-3
• 化学式: C₈H₁₀N₂O₂
• 分子量: 166.18
• InChiKey: BLMAWMUKVHMBAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  对氨基苯酚 、 氯乙酰胺 生成 D-p-hydroxyphenylglycine amide
  参考文献：
  名称：

  Lumiere; Perrin, Bulletin de la Societe Chimique de France, 1903, vol. <3>29, p. 967

  摘要：

  DOI：

文献信息

• NOVEL CRYSTALLINE CEFOPERAZONE INTERMEDIATE
  申请人：Moody Harold Monro

  公开号：US20150112057A1

  公开（公告）日：2015-04-23

  The present invention relates to a crystalline form of an intermediate for cefoperazone of formula (1) and to a process for the preparation thereof by enzymatic condensation of a 3′-thiosubstituted β-lactam nucleus with a phenylglycine derivative.

  本发明涉及一种头孢哌酮的中间体的晶型形式（化学式（1）），以及通过酶催化将3'-硫代取代的β-内酰胺核与苯基甘氨酸衍生物进行缩合制备该中间体的方法。
• Method for the preparation of enantiomerically enriched compounds
  申请人：——

  公开号：US20030097005A1

  公开（公告）日：2003-05-22

  Process for the preparation of a diasteromerically enriched phenylglycine amide derivative in which an enantomerically enriched phenylglycine amide is converted into the corresponding Schiff base with the aid of compound R 2 —C(O)—R 3, and the Schiff base obtained is subsequently converted into the diastereomerically enriched phenyglycine amide derivative with the aid of a cyanide source, a reducing agent or an allyl organometallic compound. The phenylglycine amide derivatives obtained are interesting starting materials for the preparation of for example enantimerically enriched &agr;- and or &bgr;-amino acids and derivatives thereof, such as amides and esters, and amines.

  制备对映异构体富集的苯基甘氨酸酰胺衍生物的过程，其中手性富集的苯基甘氨酸酰胺与化合物R2-C（O）-R3的帮助下转化为相应的席夫碱，随后利用氰化物源、还原剂或烯丙基有机金属化合物的帮助下将所得的席夫碱转化为对映异构体富集的苯基甘氨酸酰胺衍生物。所得到的苯基甘氨酸酰胺衍生物是制备手性富集的α-和/或β-氨基酸及其衍生物（如酰胺和酯）和胺的有趣起始材料。
• PHENYLALANINE DERIVATIVES
  申请人：Arnould Jean-Claude

  公开号：US20080045521A1

  公开（公告）日：2008-02-21

  The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.

  本发明涉及抑制a5b1功能的化合物，其制备过程，含有其作为活性成分的制药组合物，以及它们作为药物在温血动物（如人类）中治疗具有明显血管生成或血管成分的疾病，例如固体肿瘤的制药用途。本发明还涉及a5b1拮抗剂，其还表现出对其他整合素的适当选择性特征。
• Process for the preparation of an optically active amino acid amide
  申请人：DSM N.V.

  公开号：EP0442584A1

  公开（公告）日：1991-08-21

  A process for the preparation of optically active amino acid amide whereby a mixture of the L-amino and D-amino acid amides in the presence of 0.5-4 equivalents of an aldehyde, relative to the quantity of amino acid amide, in the presence of a solvent and water, is converted in whole or in part by means of an optically active carboxylic acid into a salt of the amino acid amide and the carboxylic acid, and a portion mainly consisting of one of the diastereoisomers of that salt is separated from the reaction mixture obtained. Instead of a mixture of L-amino and D-amino acid amides it is also possible to use a mixture of the Schiff bases of an amino acid amide and an aldehyde, in which case it is not necessary to add extra aldehyde, and the required quantity of water amounts to at least 1 equivalent relative to the quantity of Schiff base. With this process a high yield of optically active amino acid or the corresponding amino acid is rapidly obtained.

  一种制备光学活性氨基酸酰胺的工艺，在该工艺中，相对于氨基酸酰胺的量，在0.5-4当量的醛的存在下，在溶剂和水的存在下，L-氨基酸酰胺和D-氨基酸酰胺的混合物通过光学活性羧酸全部或部分转化为氨基酸酰胺和羧酸的盐，并从得到的反应混合物中分离出主要由该盐的非对映异构体之一组成的部分。也可以使用氨基酸酰胺和醛的席夫碱混合物来代替 L-氨基酸酰胺和 D-氨基酸酰胺混合物，在这种情况下无需额外添加醛，而且相对于席夫碱的数量，所需的水量至少为 1 个当量。通过这种工艺可以快速获得高产率的光学活性氨基酸或相应的氨基酸。
• Enzyme-catalysed preparation of optically active carboxylic acids
  申请人：DSM N.V.

  公开号：EP0494716A2

  公开（公告）日：1992-07-15

  Enzyme-catalysed preparation of an α-substituted optically active carboxylic acid, using enantioselective hydrolysis of a mixture of the enantiomers of the corresponding amide, an Ochrobactrum anthropi or an Klebsiella sp. being used as the enzyme. During the hydrolysis both the L-carboxylic acid and the remaining D-carboxylic acid amide are obtained with high optical purity and high yield, while the activity of the micro-organism is high. A large number of α-substituted carboxylic acid amides with a remarkable structural variety can be hydrolysed in this manner.

  利用酶催化法制备α-取代的光学活性羧酸，采用对映体选择性水解相应酰胺的对映体混合物，使用赭曲霉或克雷伯氏菌作为酶。在水解过程中，L-羧酸和剩余的 D-羧酸酰胺都能以高光学纯度和高产率获得，同时微生物的活性也很高。用这种方法可以水解出大量α-取代的羧酸酰胺，其结构种类繁多。