L-组氨酸乙酯盐酸盐(1:2) | 93923-84-3

• 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: L-组氨酸乙酯盐酸盐(1:2)
• 英文名称: Ethyl L-histidinate dihydrochloride
• 英文别名: ethyl (2S)-2-amino-3-(1H-imidazol-5-yl)propanoate;dihydrochloride
• CAS: 93923-84-3
• 化学式: C8H15Cl2N3O2
• mdl: MFCD00050627
• 分子量: 256.13
• InChiKey: XAWDMXNJDWMHCN-KLXURFKVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.51
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  81
• 氢给体数：
  4
• 氢受体数：
  4

安全信息

• 海关编码：
  2933290090

反应信息

• 作为反应物：
  描述：

  α-(1-naphthalenylmethyl)-1-naphthalenepropanoic acid 、 L-组氨酸乙酯盐酸盐(1:2) 、 1-羟基苯并三唑 、 三乙胺 、 N,N'-二环己基碳二亚胺 在 碳酸氢钠 、 magnesium sulfate 、 crude product 、 silica gel 、 二氯甲烷 、 methanol-dichloromethane 作用下， 以 四氢呋喃 为溶剂， 反应 16.0h， 以gave 0.15 g of the product as a white foam的产率得到(S)-3-(1H-Imidazol-4-yl)-2-(3-naphthalen-1-yl-2-naphthalen-1-ylmethyl-propionylamino)-propionic acid, ethyl ester
  参考文献：
  名称：

  Substituted dinaphthylmethyl and diheteroarylmethylacetyl histidine

  摘要：

  本文描述了公式（I）的组成为组氨酸替代物，以及其制备方法和药物组合物，其可用作蛋白酰基转移酶的抑制剂，用于治疗增生性疾病，包括癌症，再狭窄和牛皮癣，并作为抗病毒剂。 ## STR1 ##

  公开号：

  US06008372A1

文献信息

• Polyglutamic Acids Functionalised by Histidine Derivatives and Hydrophobic Groups and the Uses Thereof, in Particular for Therapeutic Purposes
  申请人：Soula Olivier

  公开号：US20100034886A1

  公开（公告）日：2010-02-11

  The invention relates to novel biodegradable materials based on modified polyamino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids. The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained to 30 carbon atoms. Said polyglutamates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorization particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7.4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.

  该发明涉及基于改性聚氨基酸的新型可生物降解材料，特别适用于载荷活性物质（AS）。该发明还涉及基于这些聚氨基酸的新型药用、化妆品、膳食或植物保护组合物。 该发明的目的是提供一种新型聚合物原料，可用于载荷AS，并能够最佳地满足该领域的所有规范要求：生物相容性、生物降解性、能够轻松与许多活性物质结合或溶解它们，并在体内释放所述活性物质。该目的在30个碳原子处实现。 通过组氨酸衍生物改性的聚谷氨酸在pH低于5时可溶解，并且可以经济地转化为能够形成稳定水性胶体悬浮液的活性物质载体颗粒。相反，这些改性聚谷氨酸在生理pH值（7.4）下不溶于水，因此在皮下注射时必须在注射部位沉淀。
• Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
  申请人：——

  公开号：US20040152888A1

  公开（公告）日：2004-08-05

  The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates. The inventive compounds more particularly correspond to general formula (I): 1

  这项发明涉及新型苯二氮卓类衍生物及其在治疗领域中的用途，特别用于治疗涉及环核苷酸磷酸二酯酶活性的病理。它还涉及制备它们的方法和新型合成中间体。这些创新化合物更特别地对应于一般式(I)：1
• pH dependent ion exchange matrix and method of use in the isolation of nucleic acids
  申请人：Promega Corporation

  公开号：US20010014650A1

  公开（公告）日：2001-08-16

  pH dependent ion exchange matrices are provided, with methods for making such matrices, and methods for using such matrices to isolate a target nucleic acid, such as plasmid DNA, chromosomal DNA, or RNA from contaminants, including proteins, lipids, cellular debris, or other nucleic acids. Each pH dependent ion exchange matrix of this invention comprises at least two different ion exchange functional groups, one of which is capable of acting as an anion exchanger at a first pH, and the other of which is capable of acting as a cation exchanger at a second, higher pH. The matrix has an overall neutral charge in a pH range between the first and second pH. The pH dependent ion exchange matrices of the present invention are designed to bind to the target nucleic acid at a pH wherein the overall charge of the matrix is positive, and to release the target nucleic acid as the pH of the surrounding solution is increased. The target nucleic acid can be released from the pH dependent matrix in little or no salt and at about a neutral pH. The matrices and methods of this invention enable one to isolate a target nucleic acid in very few steps, without the use of hazardous chemicals. Target nucleic acids isolated using the pH dependent ion exchange matrices according to the present invention can be used immediately without further extraction or isolation.

  提供了pH依赖的离子交换基质，包括制备这种基质的方法以及使用这种基质从污染物中分离目标核酸（如质粒DNA、染色体DNA或RNA）的方法，其中污染物包括蛋白质、脂质、细胞碎片或其他核酸。本发明的每个pH依赖的离子交换基质至少包含两种不同的离子交换功能基团，其中一种在第一个pH下能够作为阴离子交换剂，另一种在第二个更高的pH下能够作为阳离子交换剂。该基质在第一个和第二个pH之间的pH范围内具有总体中性电荷。本发明的pH依赖的离子交换基质被设计成在基质总体电荷为正的pH下结合目标核酸，并随着周围溶液的pH升高释放目标核酸。目标核酸可以在几乎没有盐和中性pH下从pH依赖的基质中释放出来。本发明的基质和方法使得在很少的步骤中分离目标核酸成为可能，而不需要使用危险化学品。使用本发明的pH依赖的离子交换基质分离的目标核酸可以立即使用，无需进一步提取或分离。
• process for the preparation of optically-active cyanomethyl esters
  申请人：E.I. DU PONT DE NEMOURS AND COMPANY

  公开号：EP0109681A2

  公开（公告）日：1984-05-30

  Stereoisomerically-enriched cyanomethyl esters are prepared by treating a non-symmetrical ketene or an alpha-chiral carboxylic acid halide or reactive derivative thereof with an optically-active alphahydroxynitrile. Certain optically-active optionally substituted S-alphacyano-3-phenoxybenzyl alcohol intermediates are prepared by treating the corresponding aldehyde of ketone with a source of hydrogen cyanide in the presence of a substantially water-immiscible, aprotic solvent and a cyclo(D-phenylalanyl-D-histidine) as a catalyst.

  通过将非对称酮或α-手性羧酸卤化物或其活性衍生物与具有光学活性的α-羟腈进行处理，可制备立体异构体富集的氰甲基酯。某些具有光学活性的任选取代的 S-alphacyano-3-苯氧基苄醇中间体的制备方法是：在基本上不溶于水的壬烷溶剂和作为催化剂的环(D-苯丙氨酰-D-组氨酸)存在下，用氰化氢源处理相应的酮醛。
• Preparation of optically-active alpha-substituted carboxylic esters and acids
  申请人：E.I. DU PONT DE NEMOURS AND COMPANY

  公开号：EP0116914A1

  公开（公告）日：1984-08-29

  Optically-active alpha-substituted carboxylic esters are prepared by treating a non-symmetrical ketene with an alcohol in the presence of an optically-active amine catalyst. Hydrolysis of the resulting esters, yields the optically-active acid corresponding to the non-symmetrical ketene.

  光学活性α-取代羧酸酯是通过在光学活性胺催化剂存在下用醇处理非对称酮来制备的。水解生成的酯会产生与非对 称酮相对应的光学活性酸。