ammonium hypophosphite

• 分子结构分类: 无机化合物 - 均质非金属化合物 - 非金属氧阴离子化合物
• 英文名称: ammonium hypophosphite
• 英文别名: ammonium phosphinate；Azane;phosphenous acid
• 化学式: H₄N*O₂P
• 分子量: 81.011
• InChiKey: AKYKNEHYFVLCTH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.07
• 重原子数：
  4
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  41.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  ammonium hypophosphite 、 4-甲基苄溴 在 六甲基二硅氮烷 作用下， 生成 2-[[(4-methylbenzyl)hydroxyphosphinyl]methyl]-pentanedioic acid
  参考文献：
  名称：

  Inhibitors of NAALADase enzyme activity

  摘要：

  本公开涉及二肽酶抑制剂，更特别地，涉及使用磷酸酯衍生物、羟基磷酰衍生物和磷酰胺衍生物的新方法来抑制N-乙酰化.α.-连接的酸性二肽酶（NAALADase）酶活性，并治疗前列腺疾病，特别是使用本发明的化合物抑制前列腺癌细胞生长。

  公开号：

  US06025345A1
• 作为试剂：
  描述：

  2',3'-二脱氧胸苷 在 吡啶 、 ammonium hypophosphite 、 三甲基乙酰氯 、 三乙胺 作用下， 生成 1-[(2R,5S)-5-(hydroxyphosphinothioyloxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione
  参考文献：
  名称：

  5′-Phosphonates of Ribonucleosides and 2′-Deoxyribonucleosides: Synthesis and Antiviral Activity

  摘要：

  5'-Phosphonates of natural 2'-deoxynucleosides and ribonucleosides were synthesized by condensation of 3'-O-acylated 2'-deoxynucleosides or 2',3'-substituted (2',3'-O-isopropylidene, 2',3'-O-methoxymethylene or 2',3'-O-ethoxymethylene) ribonucleosides. As condensing agents, either N,N'-dicyclohexylcarbodiimide or 2,4,6-triisopropylbenzenesulphonyl chloride were used. Nucleoside 5'-ethoxycarbonylphosphonates were converted into corresponding nucleoside 5'-aminocarbonylphosphonates by action of ammonia in methanol or aqueous ammonia. 5'-Hydrogenphosphonothioates of thymidine and 3'-deoxythymidine were obtained by reaction of phosphinic acid in the presence of pivaloyl chloride with 3'-O-acetylthymidine or 3'-deoxythymidine, respectively, followed by addition of powedered sulfur. 5'-O-methylenephosphonates of thymidine and 2'-deoxyadenosine were prepared by intramolecular reaction of corresponding 3'-O-iodomethylphosphonates under basic conditions. All compounds were tested for inhibition of several viruses, including HSV-2 and CMV, but showed no activity. A few compounds insignificantly inhibited HIV-1 reproduction. Thymidine 5'-hydrogenphosphonate neutralized anti-HIV action of 3'-azido-3'-deoxythymidine (AZT) and it indirectly showed that even some nucleoside 5'-phosphonates could be partly hydrolyzed in cell culture to corresponding nucleosides.

  DOI：

  10.1080/07328319308018558

文献信息

• .alpha.-Amino-phosphonous acids for inhibiting bacteria and yeast
  申请人：Ciba-Geigy Corporation

  公开号：US04147780A1

  公开（公告）日：1979-04-03

  The present invention relates to new phosphonous acid derivatives, especially to .alpha.-amino-phosphonous acids and processes for their production. The new phosphonous acids are valuable chemotherapeutica in the treatment of pathogenic bacteria, gram-negative bacteria and yeast.

  本发明涉及新的膦酸衍生物，特别是α-氨基膦酸及其生产过程。这些新的膦酸对治疗病原细菌、革兰氏阴性细菌和酵母等具有重要的化疗作用。
• Certain dioic acid derivatives useful as NAALADase inhibitors
  申请人：Guilford Pharmaceuticals Inc.

  公开号：US06025344A1

  公开（公告）日：2000-02-15

  The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

  本公开涉及二肽酶抑制剂，更具体地说，涉及抑制N-乙酰化α-连接酸性二肽酶（NAALADase）酶活性的新磷酸酯衍生物、羟基磷酰衍生物和磷酰胺衍生物，包括这些衍生物的药物组合物，以及使用这些衍生物抑制NAALADase活性并治疗前列腺疾病的方法，尤其是使用本发明的化合物来抑制前列腺癌细胞的生长。
• Inhibitors of NAALADase enzyme activity
  申请人：Guilford Pharmaceuticals Inc.

  公开号：US06025345A1

  公开（公告）日：2000-02-15

  The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

  本公开涉及二肽酶抑制剂，更特别地，涉及使用磷酸酯衍生物、羟基磷酰衍生物和磷酰胺衍生物的新方法来抑制N-乙酰化.α.-连接的酸性二肽酶（NAALADase）酶活性，并治疗前列腺疾病，特别是使用本发明的化合物抑制前列腺癌细胞生长。
• Pharmaceutical compositions and methods of treating compulsive disorders
  申请人：Guilford Pharmaceuticals Inc.

  公开号：US05977090A1

  公开（公告）日：1999-11-02

  The present invention relates to a pharmaceutical composition and a method for treating a compulsive disorder using a NAALADase inhibitor.

  本发明涉及一种利用NAALADase抑制剂治疗强迫症的药物组合物和方法。
• Pharmaceutical compositions and methods of treating a glutamate
  申请人：Guilford Pharmaceuticals Inc.

  公开号：US06017903A1

  公开（公告）日：2000-01-25

  The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.

  本发明涉及使用NAALADase抑制剂治疗谷氨酸异常和影响动物神经活动的方法，以及包含有效量NAALADase抑制剂的药物组合物，用于治疗动物的谷氨酸异常和影响神经活动。