4-氟-L-赖氨酸 | 742016-90-6

• 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: 4-氟-L-赖氨酸
• 英文名称: γ-fluorolysine
• 英文别名: 4-fluoro-L-lysine；(2S)-2,6-diamino-4-fluorohexanoic acid
• CAS: 742016-90-6
• 化学式: C₆H₁₃FN₂O₂
• 分子量: 164.18
• InChiKey: GVDNZQCSQRVPGZ-AKGZTFGVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.2
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  89.3
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Fluorinated cyclic hexapeptide somatostatin analogs, process for their preparation, intermediate products for their preparation and pharmaceutical compositions containing them
  申请人：Merck & Co., Inc.

  公开号：EP0104348A2

  公开（公告）日：1984-04-04

  Fluorinated somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin and the Lys side chain is monofluorinated in the γ or 8 positions. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

  氟化索马司他汀类似物的制备过程中，环状六肽含有一个仲氨基酸，取代了索马司他汀的七个环状氨基酸，赖氨酸侧链在γ或8位被单氟化。环六肽更容易合成，活性持续时间更长，而且许多环六肽的活性高于索马司他汀。这些化合物具有抑制胰高血糖素、生长激素和胰岛素释放的特性。某些化合物还能抑制胃酸分泌的释放。这些化合物尤其适用于治疗肢端肥大症、糖尿病、糖尿病视网膜病变和消化性溃疡。这些环六肽是通过固相法制备的。
• US4427661A
  申请人：——

  公开号：US4427661A

  公开（公告）日：1984-01-24
• US4602002A
  申请人：——

  公开号：US4602002A

  公开（公告）日：1986-07-22