(R)-(-)-2-氨基-6-磷酰己酸水合物

• 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: (R)-(-)-2-氨基-6-磷酰己酸水合物
• 中文别名: (R)-(-)-2-氨基-6-磷酸基己酸水合物
• 英文名称: (R)-2-Amino-6-phosphonohexanoic acid hydrate
• 英文别名: (2R)-2-amino-6-phosphonohexanoic acid;hydrate
• 化学式: C6H16NO6P
• 分子量: 229.17
• InChiKey: CFYNRRACSWVRFN-NUBCRITNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.08
• 重原子数：
  14
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  122
• 氢给体数：
  5
• 氢受体数：
  7

文献信息

• OPTICALLY-ACTIVE 2-AMINO-PHOSPHONOALKANE ACID, OPTICALLY-ACTIVE 2-AMINOPHOSPHONOALKANE ACID SALT, AND HYDRATES OF THESE
  申请人：NAHLS CORPORATION CO., LTD.

  公开号：US20200131207A1

  公开（公告）日：2020-04-30

  A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

  一种新的化合物具有与Nahlsgen相媲美的药理活性，并且具有出色的稳定性。该化合物可以通过根据本发明用于生产光学活性2-氨基磷酸酯盐的方法来生产。在该方法中，以式（1）表示的起始材料DL-2-氨基磷酸酯或其水合物与光学活性的碱性化合物（不包括光学活性赖氨酸）发生反应，形成一个不对映异构盐混合物，其中包括D-2-氨基磷酸酯（式（1-1）表示）和光学活性碱性化合物之间的第一盐（包括水合盐），以及L-2-氨基磷酸酯（式（1-2）表示）和光学活性碱性化合物之间的第二盐（包括水合盐）。将不对映异构盐混合物进行分级结晶以分离第一和第二不对映异构盐中的一种。
• OPTICALLY-ACTIVE 2-AMINO-PHOSPHONOALKANE ACID, OPTICALLY-ACTIVE 2-AMINO-PHOSPHONOALKANE ACID SALT, AND HYDRATES OF THESE
  申请人：Kyoto University

  公开号：EP3613750A1

  公开（公告）日：2020-02-26

  A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

  一种新型化合物具有与Nahlsgen相当的药理活性，并具有极佳的稳定性。根据本发明生产光学活性 2-氨基膦酰基烷酸盐的方法，可以生产出该化合物。在该方法中，由式（1）代表的起始原料 DL-2-氨基膦酰基烷酸或其水合物与光学活性赖氨酸以外的光学活性碱性化合物反应、得到非对映异构盐混合物，包括由式（1-1）代表的 D-2-氨基膦酰基烷酸和光学活性碱性化合物之间的第一种盐（包括水合盐），以及由式（1-2）代表的 L-2-氨基膦酰基烷酸和光学活性碱性化合物之间的第二种盐（包括水合盐）。非对映异构盐混合物经分馏结晶，分离出第一和第二非对映异构盐中的一种。
• WOUND HEALING PROMOTER
  申请人：Nahls Corporation Co., Ltd.

  公开号：EP3613422A1

  公开（公告）日：2020-02-26

  A pharmaceutical preparation efficaciously promotes tissue wound repair. The wound repair promoter according to the present invention includes at least one active ingredient selected from the group consisting of compounds represented by Formula (1), salts of the compounds, and hydrates of the compounds or the salts. In the formula, R1 and R2 are each, identically or differently, selected from hydrogen and a hydrocarbon group optionally having one or more substituents selected from the group consisting of halogens, -COOR3, -CONR32, -COR3, -CN, -NO2, -NHCOR3, -OR3,-SR3, -OCOR3, -SO3R3, and -SO2NR32, where R3 is, identically or differently in each occurrence, selected from hydrogen and an optionally substituted aliphatic hydrocarbon group; and n represents an integer of 1 or more.

  一种能有效促进组织伤口修复的药物制剂。根据本发明的伤口修复促进剂包括至少一种活性成分，该活性成分选自由式（1）表示的化合物、化合物的盐、化合物或盐的水合物组成的组。在式中，R1和R2各自相同或不同地选自氢和任选具有一个或多个取代基的烃基，这些取代基选自由卤素、-COOR3、-CONR32、-COR3、-CN、-NO2、-NHCOR3、-OR3、-SR3、-OCOR3、-SO3R3和-SO2NR32组成的组；其中R3在每次出现时相同或不同地选自氢和任选取代的脂肪族烃基；n代表1或更多的整数。
• Wound healing promoter
  申请人：NAHLS CORPORATION CO., LTD.

  公开号：US11090318B2

  公开（公告）日：2021-08-17

  A pharmaceutical preparation efficaciously promotes tissue wound repair. The wound repair promoter according to the present invention includes at least one active ingredient selected from the group consisting of compounds represented by Formula (1), salts of the compounds, and hydrates of the compounds or the salts. In the formula, R1 and R2 are each, identically or differently, selected from hydrogen and a hydrocarbon group optionally having one or more substituents selected from the group consisting of halogens, —COOR3, —CONR32, —COR3, —CN, —NO2, —NHCOR3, —OR3, —SR3, —OCOR3, —SO3R3, and —SO2NR32, where R3 is, identically or differently in each occurrence, selected from hydrogen and an optionally substituted aliphatic hydrocarbon group; and n represents an integer of 1 or more.

  一种能有效促进组织伤口修复的药物制剂。根据本发明的伤口修复促进剂包括至少一种活性成分，该活性成分选自由式（1）表示的化合物、化合物的盐、化合物或盐的水合物组成的组。在式中，R1和R2各自相同或不同地选自氢和任选具有一个或多个选自卤素、-COOR3、-CONR32、-COR3、-CN、-NO2、-NHCOR3、-OR3、-SR3、-OCOR3、-SO3R3和-SO2NR32组成的组的取代基的烃基，其中R3在每次出现时相同或不同地选自氢和任选取代的脂肪族烃基；n代表1或更多的整数。
• Optically-active 2-amino-phosphonoalkane acid, optically-active 2-amino-phosphonoalkane acid salt, and hydrates of these
  申请人：NAHLS CORPORATION CO., LTD.

  公开号：US11220521B2

  公开（公告）日：2022-01-11

  A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

  一种新型化合物具有与Nahlsgen相当的药理活性，并具有极佳的稳定性。根据本发明生产光学活性 2-氨基膦酰基烷酸盐的方法，可以生产出该化合物。在该方法中，由式（1）代表的起始原料 DL-2-氨基膦酰基烷酸或其水合物与光学活性赖氨酸以外的光学活性碱性化合物反应、得到非对映异构盐混合物，包括由式（1-1）代表的 D-2-氨基膦酰基烷酸和光学活性碱性化合物之间的第一种盐（包括水合盐），以及由式（1-2）代表的 L-2-氨基膦酰基烷酸和光学活性碱性化合物之间的第二种盐（包括水合盐）。非对映异构盐混合物经分馏结晶，分离出第一和第二非对映异构盐中的一种。