sodium;chloro-(4-methylphenyl)sulfonylazanide;trihydrate

• 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: sodium;chloro-(4-methylphenyl)sulfonylazanide;trihydrate
• 化学式: C7H13ClNNaO5S
• 分子量: 281.69
• InChiKey: NZYOAGBNMCVQIV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.26
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  46.5
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  sodium;chloro-(4-methylphenyl)sulfonylazanide;trihydrate 、 4-硝基茴香硫醚 在 乙酸乙酯 、 Sodium sulfate-III 、 甲醇 作用下， 以 乙腈 、 乙酸乙酯 为溶剂， 反应 4.0h， 以2.2 g (6.5 mmol; yield: 22%) of the product are obtained的产率得到4-methyl-N-(methyl(4-nitrophenyl)-λ⁴-sulfaneylidene)benzenesulfonamide
  参考文献：
  名称：

  SULPHIMIDES AS PROTEIN KINASE INHIBITORS

  摘要：

  本发明涉及通式I的硫代酰胺作为蛋白激酶抑制剂。

  公开号：

  US20080058358A1

文献信息

• Bicyclic signal transduction inhibitors, compositions containing them & uses thereof
  申请人：——

  公开号：US20020062031A1

  公开（公告）日：2002-05-23

  This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula 1 as defined herein.

  本发明涉及用于抑制细胞内信号转导的化合物，特别是介导涉及磷酸酪氨酸含有蛋白质的一种或多种分子相互作用的细胞内信号转导。本发明还涉及含有该化合物的药物组合物以及涉及药物和兽医管理的预防和治疗方法。该化合物的公式1如本文所定义。
• BICYCLIC SIGNAL TRANSDUCTION INHIBITORS, COMPOSITIONS CONTAINING THEM & USES THEREOF
  申请人：——

  公开号：US20020137941A1

  公开（公告）日：2002-09-26

  This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula 1 as defined herein.

  本发明涉及用于抑制细胞内信号转导的化合物，特别是介导涉及磷酸酪氨酸含有蛋白质的一个或多个分子相互作用的细胞内信号转导。本发明还涉及含有该化合物的药物组合物以及使用该化合物进行药物和兽医治疗的预防和治疗方法。该化合物的公式1如定义所述。
• Two step synthesis of D- and L- .alpha.-amino acids and D- and L-
  申请人：The Scripps Research Institute

  公开号：US05994583A1

  公开（公告）日：1999-11-30

  D- and L-.alpha.-amino acids and D- and L-.alpha.-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant .beta.-hydroxycarbamate is deprotected to yield the corresponding .beta.-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant .beta.-hydroxysulfonamide is deprotected to yield the corresponding .beta.-hydroxyamine. The resultant .beta.-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L-.alpha.-amino acid or D- and L-.alpha.-amino aldehyde.

  D-和L-.alpha.-氨基酸和D-和L-.alpha.-氨基醛可以通过两个步骤从烯烃底物合成。第一步是催化不对称氨羟化加成反应到烯烃底物。加成反应由钌催化，并由手性配体共催化。手性配体除了与钌一起作为共催化剂外，还能以立体选择性和对区域选择性引导加成反应。双价配体比单价配体更受欢迎，因为它们具有更强的区域和对映选择性。作为加成反应的氮氧化剂，可以使用羰酸酯或磺酰胺。如果使用羰酸酯作为氮氧化剂，生成的β-羟基羰酸酯将去保护后产生相应的β-羟基胺。如果使用磺酰胺作为氮氧化剂，生成的β-羟基磺酰胺将去保护后产生相应的β-羟基胺。然后在第二个合成步骤中选择性地氧化生成所需的D-和L-.alpha.-氨基酸或D-和L-.alpha.-氨基醛。
• Spiro-piperidine derivatives and their use as therapeutic agents
  申请人：Merck Sharp & Dohme Ltd.

  公开号：US06071927A1

  公开（公告）日：2000-06-06

  The present invention relates to certain spiro-piperdine derivatives which are tachykinnin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

  本发明涉及某些螺环哌啶衍生物，它们是快速肽激动剂拮抗剂，例如，它们在治疗或预防疼痛、炎症、偏头痛、恶心和带状疱疹后神经痛方面是有用的。
• Catalytic asymmetric aminohydroxylation of olefins with sulfonamides
  申请人：The Scripps Research Institute

  公开号：US05859281A1

  公开（公告）日：1999-01-12

  .beta.-Hydroxyamines and .beta.-hydroxysulfonamides are synthesized from olefin substrates by means on a catalyzed asymmetric addition reaction. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. Sulfonamides are employed as an oxidant nitrogen source for the production of .beta.-hydroxysulfonamides. Excellent yields and enantiomeric efficiencies are achieved with co-solvents containing a 50/50 (v/v) mixtures of water and organic solvent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxysulfonamides.

  .beta.-羟基胺和.beta.-羟基磺酰胺是通过催化不对称加成反应从烯烃底物合成的。加成反应由钌催化，并由手性配体共同催化。除了与钌一起作为共催化剂外，手性配体还用于选择性地定向加成反应的位置和对映选择性。二价配体比单价配体更受欢迎，因为它们具有更强的位置和对映选择性。磺酰胺被用作氧化剂氮源，用于生产.beta.-羟基磺酰胺。在含有50/50（体积比）的水和有机溶剂混合物的共溶剂中，可实现优异的产率和对映效率。通过去保护相应的.beta.-羟基磺酰胺获得.beta.-羟基胺。