L-dehydroascorbic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酯类
• 英文名称: L-dehydroascorbic acid
• 英文别名: dihydroascorbic acid；ascorbic acid；3H2P；(5R)-5-[(1S)-1,2-dihydroxyethyl]-3,4-dihydroxyoxolan-2-one
• 化学式: C₆H₁₀O₆
• 分子量: 178.142
• InChiKey: SXZYCXMUPBBULW-FORAYFFESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  107
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  维生素 C 在 actinorhodin 作用下， 以 aq. phosphate buffer 为溶剂， 生成 L-dehydroascorbic acid
  参考文献：
  名称：

  10.1073/pnas.1417941111/-/dcsupplemental

  摘要：

  DOI：

  10.1073/pnas.1417941111/-/dcsupplemental
• 作为试剂：
  描述：

  5-氟-DL-色氨酸 在 recombinant human indoleamine 2,3-dioxygenase 、 亚甲兰 、 L-dehydroascorbic acid 、 bovine liver catalase 作用下， 以 aq. phosphate buffer 为溶剂， 反应 0.5h， 生成
  参考文献：
  名称：

  Human indoleamine 2,3-dioxygenase-2 has substrate specificity and inhibition characteristics distinct from those of indoleamine 2,3-dioxygenase-1

  摘要：

  Indoleamine 2,3-dioxygenase-2 (IDO2) is one of three enzymes (alongside tryptophan 2,3-dioxygenase and indoleamine 2,3-dioxygenase (IDO1)) that catalyse dioxygenation of L-tryptophan as the first step in the kynurenine pathway. Despite the reported expression of IDO2 in tumours, some fundamental characteristics of the enzyme, such as substrate specificity and inhibition selectivity, are still to be clearly defined. In this study, we report the kinetic and inhibition characteristics of recombinant human IDO2. Choosing from a series of likely IDO2 substrates, we screened 54 tryptophan derivatives and tryptophan-like molecules, and characterised the 8 with which the enzyme was most active. Specificity of IDO2 for the two isomers of 1-methyltryptophan was also evaluated and the findings compared with those obtained in other studies on IDO2 and IDO1. Interestingly, IDO2 demonstrates behaviour distinct from that of IDO1 in terms of substrate specificity and affinity, such that we have identified tryptophan derivatives that are mutually exclusive as substrates for IDO1 and IDO2. Our results support the idea that the antitumour activity of 1-Me-D-Trp is unlikely to be related with competitive inhibition of IDO2, and also imply that there are subtle differences in active site structure in the two enzymes that may be exploited in the development of specific inhibitors of these enzymes, a route which may prove important in defining their role(s) in cancer.

  DOI：

  10.1007/s00726-014-1766-3

文献信息

• [EN] BIARYL PYRAZOLES AS NRF2 REGULATORS<br/>[FR] BIARYL PYRAZOLES UTILISÉS COMME RÉGULATEURS DE NRF2
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2017060854A1

  公开（公告）日：2017-04-13

  The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

  本发明涉及双芳基吡唑化合物、它们的制备方法、含有它们的药物组合物及其作为NRF2调节剂的应用。
• [EN] METHOD FOR THE SYNTHESIS OF 4-ALKOXY-, 4-HYDROXY- AND 4-ARYLOXY-SUBSTITUTED TETRAHYDRO-FURO[3,4-B]FURAN-2(3H)-ONE COMPOUNDS<br/>[FR] PROCÉDÉ DE SYNTHÈSE DE COMPOSÉS DE TÉTRAHYDRO-FURO[3,4-B]FURAN-2(3H)-ONE SUBSTITUÉS 4-ALKOXY-, 4-HYDROXY- AND 4-ARYLOXY
  申请人：DSM IP ASSETS BV

  公开号：WO2009030733A1

  公开（公告）日：2009-03-12

  The present invention relates to a method for the synthesis of enantiomerically and diastereomerically enriched 4-alkoxy-, 4-hydroxy- or 4-aryloxy- substituted tetrahydro-furo[3,4-b]furan-2(3H)-ones by aldol coupling of a suitable hydroxyl-protected hydroxy-acetaldehyde and 4-oxobutanoic acid or an ester thereof, and subsequent removal of the protecting group from the aldol compound and (optionally simultaneous) cyclizations and acetal formation under acidic conditions in the presence of an alcohol, followed by optional isolation of the desired compounds. The invention also relates to compounds according to formulae [Xl] and [XII].

  本发明涉及一种通过适当的羟基保护羟基乙醛和4-氧代丁酸或其酯的醛缩合，以及随后去除醛缩合物中的保护基并在酸性条件下进行（可选同时进行）环化和缩醛形成的方法，从而合成对映体和对映体富集的4-烷氧基、4-羟基或4-芳氧基取代的四氢呋喃并[3,4-b]呋喃-2(3H)-酮，随后可选择地分离所需的化合物。该发明还涉及符合[XI]和[XII]式的化合物。
• PROCESS FOR TRANSFORMING THE END GROUPS OF POLYMERS
  申请人：Moad Graeme

  公开号：US20100137548A1

  公开（公告）日：2010-06-03

  The present invention is directed to a process for the cleavage of one or more starting polymers having thiocarbonylthio groups of the formula (I) into derived polymers in which the —S—(C═S)— group is transformed. The process includes contacting the starting polymer containing groups Y b with one or more reagents containing groups X a to produce the derived polymer and a byproduct containing the groups Y b , wherein the groups X a is one or more reactive groups and the groups Y b is an extracting group and a byproduct, which is then separated from the derived polymer by conventional separation processes. The derived polymer is free from odor or color that is sometimes associated with the starting polymer and it can be used in making optical lenses, such as high refractive index spectacle lenses.

  本发明涉及一种将具有硫代氨基甲酸酯基团的一个或多个起始聚合物通过裂解转化为衍生聚合物的方法，其中的—S—(C═S)—基团得到转化。该方法包括将含有Yb基团的起始聚合物与含有Xa基团的一种或多种试剂接触，以生成衍生聚合物和一种含有Yb基团的副产物，其中Xa基团是一种或多种反应性基团，而Yb基团是一种提取基团和副产物，然后通过常规分离工艺将衍生聚合物与副产物分离。衍生聚合物没有起始聚合物所具有的气味或颜色，并可用于制造光学透镜，如高折射率眼镜镜片。
• Biaryl pyrazoles as NRF2 regulators
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US10364256B2

  公开（公告）日：2019-07-30

  The present invention relates to biaryl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

  本发明涉及式（I）的双芳基吡唑化合物 的制造方法、含有它们的药物组合物以及它们作为 NRF2 调节剂的用途。
• Process for synthesizing thiol terminated polymers
  申请人：Moad Graeme

  公开号：US20070232783A1

  公开（公告）日：2007-10-04

  The present invention is directed to a process for the cleavage of one or more starting polymers having thiocarbonylthio groups of the formula —S—(C═S)— into derived polymers having thiol end groups of the formula —SH. The process includes contacting the aforedescribed starting polymers, with a reagent having the formula X a Y b , wherein X a is a nucleophilic group and Y b is an extracting group that results in the starting polymer and a byproduct, which is then separated from the derived polymer by conventional separation processes. The derived polymer is free from any odor or color that is sometimes associated with the starting polymer and it can be used in making optical lenses, such as contact lenses.