N^α-p-tosyl-L-arginine | 1159-15-5

• 物质功能分类: 生物化工 - 氨基酸及其衍生物 - 精氨酸类衍生物
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N^α-p-tosyl-L-arginine
• 英文别名: p-tosyl-L-arginine；tosyl-L-arginine；TAOH；N^α-(toluene-4-sulfonyl)-L-arginine；N^α-(Toluol-4-sulfonyl)-L-arginin；N^α-(Toluol-sulfonyl-(4))-L-arginin；(2S)-5-(diaminomethylideneazaniumyl)-2-[(4-methylphenyl)sulfonylamino]pentanoate
• CAS: 1159-15-5
• 化学式: C₁₃H₂₀N₄O₄S
• mdl: MFCD00019732
• 分子量: 328.392
• InChiKey: KFNRNFXZFIRNEO-NSHDSACASA-N

物化性质

• 溶解度：
  溶于氯仿、二氯甲烷、乙酸乙酯、DMSO、丙酮等。

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  22
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  156
• 氢给体数：
  4
• 氢受体数：
  6

安全信息

• 危险等级：
  IRRITANT
• 危险品标志：
  Xi
• 安全说明：
  S24/25,S26,S3/9/14,S30,S36/37,S37/39,S45,S61
• 危险类别码：
  R36/37/38
• 海关编码：
  2935009090
• 危险类别：
  4.3
• 包装等级：
  I
• 危险品运输编号：
  1397
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  N^α-p-tosyl-L-arginine 在 氢溴酸 、 溶剂黄146 、 苯酚 作用下， 生成 L-精氨酸
  参考文献：
  名称：

  Zaoral; Rudinger, Collection of Czechoslovak Chemical Communications, 1959, vol. 24, p. 1993,2002

  摘要：

  DOI：
• 作为产物：
  描述：

  NA-P-甲苯磺酰-L-精氨酸甲酯盐酸盐 在 Tris-HCl buffer 、 Thunnus tonggol spleen trypsin 作用下， 反应 0.33h， 生成 N^α-p-tosyl-L-arginine
  参考文献：
  名称：

  Purification and Characterization of Trypsin from the Spleen of Tongol Tuna (Thunnus tonggol)

  摘要：

  Trypsin from tongol tuna (Thunnus tonggol) spleen was purified to 402-fold by ammonium sulfate precipitation, followed by a series of chromatographic separations. The molecular mass of trypsin was estimated to be 24 kDa by size-exclusion chromatography and sodium dodecyl sulfate-polyacrylamide gel electrophoresis ( SDS- PAGE). Trypsin appearing as a single band on native PAGE showed the maximal activity at pH 8.5 and 65 degrees C. It was stable in a wide pH range of 6-11 but unstable at the temperatures greater than 50 degrees C. The enzyme required calcium ion for thermal stability. The activity was strongly inhibited by 1.0 g/L soybean trypsin inhibitor and 5 mM TLCK and partially inhibited by 2 mM ethylenediaminetetraacetic acid. Activity was lowered with an increasing NaCl concentration (0-30%). The enzyme had a K-m for N-alpha-p-tosyl-L-arginine methyl ester hydrochloride of 0.25 mM and a K cat of 200 s(-1). The N-terminal amino acid sequence of trypsin was determined as IVGGYECQAHSQPHQVSLNA and was very homologous to other trypsins.

  DOI：

  10.1021/jf060699d

文献信息

• [EN] REDOX DEHYDRATION COUPLING CATALYSTS AND METHODS RELATED THERETO<br/>[FR] CATALYSEURS DE COUPLAGE DE DÉSHYDRATATION RÉDOX ET PROCÉDÉS ASSOCIÉS À CEUX-CI
  申请人：UNIV EMORY

  公开号：WO2017070157A1

  公开（公告）日：2017-04-27

  This disclosure relates to synthetic coupling methods using catalytic molecules. In certain embodiments, the catalytic molecules comprise heterocyclic thiolamide, S-acylthiosalicylamide, disulfide, selenium containing heterocycle, diselenide compound, ditelluride compound or tellurium containing heterocycle. Catalytic molecules disclosed herein are useful as catalysts in the transformation of hydroxy group containing compounds to amides, esters, ketones, and other carbon to heteroatom or carbon to carbon transformations.

  这份披露涉及使用催化分子的合成偶联方法。在某些实施例中，这些催化分子包括杂环硫酰胺、S-酰基硫代水杨酰胺、二硫化物、含硒杂环、二硒化合物、二碲化合物或含碲杂环。本文披露的催化分子可用作催化剂，用于将含羟基化合物转化为酰胺、酯、酮和其他碳到杂原子或碳到碳的转化过程中。
• Urea derivative, process for producing the same, and use
  申请人：Kubo Keiji

  公开号：US20070093501A1

  公开（公告）日：2007-04-26

  The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis. The derivative is represented by Formula (I): wherein Cy is an aromatic hydrocarbon group which may be substituted or an aromatic heterocyclic group which may be substituted; R 1 is a hydrogen atom or a hydrocarbon group which may be substituted; V is —C(O)—, —S(O)—, or —S(O) 2 —; W is —N(R 2 )—, —O—, or a bond (wherein R 2 is a hydrogen atom or a hydrocarbon group which may be substituted); X is alkylene which may be substituted; Y is —C(O)—, —S(O)—, or —S(O) 2 —; Z is a bond, a chain hydrocarbon group which may be substituted, or —N═; ring A is a non-aromatic nitrogen-containing heterocyclic ring which may be substituted; ring B is a nitrogen-containing heterocyclic ring which may be substituted; and [Chemical formula 2] , are each independently a single bond or a double bond; provided that R 1 may be bonded to R 2 to form a non-aromatic nitrogen-containing heterocyclic ring and that R 2 may be bonded to a substituent of X to form a non-aromatic nitrogen-containing heterocyclic ring which may be substituted.

  本发明提供一种尿素衍生物或其盐，其作为治疗血栓症的治疗剂是有用的。该衍生物由公式（I）表示：其中，Cy是芳香族羟基烃基或芳香族杂环基，可以被取代；R1是氢原子或可以被取代的碳氢基团；V是-C（O）-，-S（O）-或-S（O）2-；W是-N（R2）-，-O-或键（其中R2是氢原子或可以被取代的碳氢基团）；X是可以被取代的烷基；Y是-C（O）-，-S（O）-或-S（O）2-；Z是键，可以被取代的链烃基团或-N═；环A是非芳香族含氮杂环环，可以被取代；环B是含氮杂环环，可以被取代；而[化学式2]都是单键或双键；但是，R1可以与R2连接形成非芳香族含氮杂环环，而R2可以与X的取代基连接形成可以被取代的非芳香族含氮杂环环。
• Method of Producing Peptide
  申请人：Murao Hiroshi

  公开号：US20090069538A1

  公开（公告）日：2009-03-12

  The present invention is related to a method of producing a peptide, characterized in contacting a reaction mixture with a base after a condensation reaction to hydrolyze while a basic condition is maintained until a ratio of a remaining unreacted active ester of an acid component is decreased to 1% or less in a liquid phase peptide synthesis method. According to the invention, a target peptide of high purity can be simply and efficiently produced by a continuous liquid phase synthesis method. Further, the present invention is related to a method of producing a peptide, characterized in using an amide-type solvent immiscible with water in a liquid phase peptide synthesis method. According to the invention, various peptides can be produced by the liquid phase synthesis method without being restricted by the amino acid sequence of the target peptide.

  本发明涉及一种肽的制备方法，其特征在于，在缩合反应后将反应混合物与碱接触以水解，同时保持碱性条件，直到酸组分的剩余未反应活性酯的比例在液相肽合成方法中降至1％以下。根据本发明，可以通过连续的液相合成方法简单高效地生产高纯度的目标肽。此外，本发明涉及一种肽的制备方法，其特征在于，在液相肽合成方法中使用与水不相溶的酰胺型溶剂。根据本发明，可以通过液相合成方法生产各种肽，而不受目标肽氨基酸序列的限制。
• [EN] HETEROCYCLIC COUPLING CATALYSTS AND METHODS RELATED THERETO<br/>[FR] CATALYSEURS DE COUPLAGE HÉTÉROCYCLIQUE ET PROCÉDÉS ASSOCIÉS À CEUX-CI
  申请人：UNIV EMORY

  公开号：WO2015054337A1

  公开（公告）日：2015-04-16

  This disclosure relates to synthetic coupling methods using a catalytic molecule comprising two bonded atoms wherein one atom is an amide nitrogen and the second atom is not nitrogen or carbon, such as sulfur, such as a sufur amide nitrogen bond, typically in a heterocycle, such as substituted benzoisothiazolones and derivatives thereof, as a catalyst in the transformation of hydroxy group containing compounds to amides, esters, ketones, and other carbon to heteroatom or carbon to carbon transformations.

  本披露涉及使用催化分子的合成偶联方法，其中该催化分子包含两个键合原子，其中一个原子是酰胺氮，第二个原子不是氮或碳，例如硫，例如硫酰胺氮键，通常在杂环中，例如取代苯并异噻唑酮及其衍生物，用作催化剂将含羟基的化合物转化为酰胺，酯，酮和其他碳到杂原子或碳到碳的转化。
• Piperazine derivatives and processes for producing them
  申请人：KOWA COMPANY, LTD.

  公开号：EP0067561A2

  公开（公告）日：1982-12-22

  Novel piperazine derivatives represented by the following formula: wherein R, is an indolyl group which may optionally be substituted by one or more lower alkyl and/or lower alkoxy groups, a naphthyl group which may optionally be partially saturated with 2 or 4 hydrogen atoms, or a phenyl or cyclohexyl group which may optionally be substituted by one or more lower alkyl groups; A is a single bond or an alkylene group; P is a single bond or a vinylene group; Q is an -O-alkylene group or an -NH-alkylene group when P is a single bond, or a single bond when P is a vinylene group; and R2 is a lower alkyl, morpholino-lower alkyl, morpholinocarbonyl lower alkyl, piperidinocarbonyl lower alkyl, piperazinocarbonyl lower alkyl or lower alkylaminocarbonyl lower alkyl group, and acid addition salts thereof are described, which are proteolytic enzyme inhibitors. Processes for preparing the novel derivatives are described.

  下式所代表的新型哌嗪衍生物： 其中 R，是吲哚基，可任选被一个或多个低级烷基和/或低级烷氧基取代；R，是萘基，可任选被 2 个或 4 个氢原子部分饱和；R，是苯基或环己基，可任选被一个或多个低级烷基取代； A 是单键或亚烷基； P 是单键或乙烯基； Q 是-O-亚烷基或-NH-亚烷基（当 P 为单键时），或单键（当 P 为乙烯基时）；以及 R2 是低级烷基、吗啉低级烷基、吗啉羰基低级烷基、哌啶羰基低级烷基、哌嗪羰基低级烷基或低级烷基氨基羰基低级烷基、 及其酸加成盐，它们是蛋白水解酶抑制剂。还介绍了制备这些新型衍生物的工艺。