diethyl 1-(R)-amino-3-phenylpropylphosphonate | 164202-35-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机膦酸及其衍生物
• 英文名称: diethyl 1-(R)-amino-3-phenylpropylphosphonate
• 英文别名: (1R)-1-diethoxyphosphoryl-3-phenylpropan-1-amine
• CAS: 164202-35-1
• 化学式: C₁₃H₂₂NO₃P
• 分子量: 271.296
• InChiKey: UTFOOCIMFKVUFN-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  18
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  61.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  diethyl 1-(R)-amino-3-phenylpropylphosphonate 、 benzyl 2R-trifluoromethanesulfonyloxy-4-methylvalerate 在 三乙胺 作用下， 以 二氯甲烷 、 水 为溶剂， 生成 N-(1-diethoxyphosphoryl-3-phenylpropyl)-leucine benzyl ester
  参考文献：
  名称：

  Aminophosphonic acid derivative

  摘要：

  提供了一种新型的氨基膦酸衍生物，其一般式如下[I]：其中n是2或3的整数；R¹是苯基，萘基，吲哚基，苯并噻吩基，苯并呋喃基或苯并噁唑基，其可具有1至3个取自氢氧基和低烷氧基的取代基，或是氢原子；R²是低烷基，苄基，4-羟基苄基，3-吲哚甲基基或β-苯乙基；A是选自色氨酸，酪氨酸，苯丙氨酸，同型苯丙氨酸，萘氨酸或Nω-硝基精氨酸的氨基酸残基，以及它们的药学上可接受的盐。根据本发明的化合物及其药学上可接受的盐表现出对内皮素转化酶的抑制活性，预计可用于治疗与内皮素相关的各种疾病的药物。

  公开号：

  EP0623625A1

文献信息

• Aminophosponic acid derivative
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US05380921A1

  公开（公告）日：1995-01-10

  There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

  提供了一种一般式[I]的新型氨基膦酸衍生物：其中n是2或3的整数；R.sup.1是苯基、萘基、吲哚基、苯并噻吩基、苯并呋喃基或苯并噁唑基，可能具有1至3个亚羟基和较低的烷氧基从羟基和较低的烷氧基中选择的取代基，或氢原子；R.sup.2是较低的烷基、苄基、4-羟基苄基、3-吲哚甲基基团或β-苯乙基基团；A是从色氨酸、酪氨酸、苯丙氨酸、同苯丙氨酸、萘丙氨酸或N.ω.-硝基精氨酸中选择的氨基酸的可选残基和它们的药用盐。根据本发明的化合物及其药用盐对内皮素转化酶表现出抑制活性，并有望作为治疗涉及内皮素的各种疾病的药物。
• US5380921A
  申请人：——

  公开号：US5380921A

  公开（公告）日：1995-01-10
• Aminophosphonic acid derivative
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP0623625A1

  公开（公告）日：1994-11-09

  There are provided novel aminophosphonic acid derivatives of the general formula [I]: wherein n is an integer of 2 or 3; R¹ is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R² is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a β-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or Nω-nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

  提供了一种新型的氨基膦酸衍生物，其一般式如下[I]：其中n是2或3的整数；R¹是苯基，萘基，吲哚基，苯并噻吩基，苯并呋喃基或苯并噁唑基，其可具有1至3个取自氢氧基和低烷氧基的取代基，或是氢原子；R²是低烷基，苄基，4-羟基苄基，3-吲哚甲基基或β-苯乙基；A是选自色氨酸，酪氨酸，苯丙氨酸，同型苯丙氨酸，萘氨酸或Nω-硝基精氨酸的氨基酸残基，以及它们的药学上可接受的盐。根据本发明的化合物及其药学上可接受的盐表现出对内皮素转化酶的抑制活性，预计可用于治疗与内皮素相关的各种疾病的药物。