5,5'-dihydroxyleucine | 70461-91-5

• 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
• 英文名称: 5,5'-dihydroxyleucine
• 英文别名: DL-5,5'-Dihydroleucin；2-Amino-5-hydroxy-4-(hydroxymethyl)pentanoic acid
• CAS: 70461-91-5
• 化学式: C₆H₁₃NO₄
• 分子量: 163.174
• InChiKey: ULPQPOGKWRDOJK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4
• 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：
  104
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2,2-dimethyl-5-(2'-carbethoxy-2'diphenylmethylimino-ethane)-1,3-dioxane 在 盐酸 作用下， 反应 4.0h， 以57%的产率得到5,5'-dihydroxyleucine
  参考文献：
  名称：

  Synthesis of 5,5′-dihydroxyleucine and 4-fluoro 5,5′-dihydroxyleucine, the reduction products of 4-carboxyglutamic and 4-carboxy-4-fluoroglutamic acids

  摘要：

  Schemes for the synthesis of 5-5'-dihydroxyleucine 3 and its 4-fluoro analog 7 involving the condensation of a suitable ''aminoacid moiety'' with 2,2-dimethyl-5-iodomethyl-1,3-dioxane 15D or its fluoro analog 27A were tested. The anion of the ethyl N-diphenylmethylene-glycinate 25 gave better yields of 3 than the classical anion of diethyl acetamidomalonate. This strategy could not be successfully applied to the synthesis of 7, which could be prepared by reduction of a suitably protected 4-fluoro-4-carboxyglutamate with BMS.

  DOI：

  10.1016/s0040-4020(01)80939-x

文献信息

• Inhibitors of hepatitis C virus NS3 protease
  申请人：——

  公开号：US20020065248A1

  公开（公告）日：2002-05-30

  The present invention relates to compounds of Formula (I): 1 wherein A 1 is methylene, ethylene or propylene group and A 2 is N or CR 5 , or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

  本发明涉及化合物的结构公式（I）：其中A1为亚甲基、乙烯基或丙烯基，A2为N或CR5，或其立体异构体形式、立体异构体混合物或药用盐形式，用作HCV NS3蛋白酶的抑制剂，以及包含相同化合物的药物组合物和诊断试剂盒，以及用于治疗病毒感染或作为测定标准或试剂的方法。
• Peptide inhibitors of hepatitis C virus NS3 protein
  申请人：——

  公开号：US20020177725A1

  公开（公告）日：2002-11-28

  This invention relates to a novel class of peptides having the Formula (I): 1 Which are useful as serine protease inhibitors, and more particularly as Hepatitis C virus(HCV) NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same in the treatment of HCV infection.

  本发明涉及一类新型肽的公式(I)：1，其作为丝氨酸蛋白酶抑制剂具有用途，更具体地作为丙型肝炎病毒（HCV）NS3蛋白酶抑制剂。本发明还涉及包含这些化合物的制药组合物以及使用它们治疗HCV感染的方法。
• AMIDINO AND GUANIDINO SUBSTITUTED INHIBITORS OF TRYPSIN-LIKE ENZYMES
  申请人：THE DU PONT MERCK PHARMACEUTICAL COMPANY

  公开号：EP0787010A1

  公开（公告）日：1997-08-06
• PEPTIDE BORONIC ACID INHIBITORS OF HEPATITIS C VIRUS PROTEASE
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：EP1196436A2

  公开（公告）日：2002-04-17
• Therapeutic compositions and methods using transforming growth factor-beta mimics
  申请人：Bhatnagar S. Rajendra

  公开号：US20060293228A1

  公开（公告）日：2006-12-28

  The invention provides methods, compositions, and kits for treating a variety of conditions using substances that display one or more activities of transforming growth factor-β (TGF-β mimics). Conditions include skin conditions, wounds, and the need for soft tissue augmentation. Compositions that may be used to treat such conditions contain a TGF-β mimic. Kits that may be used to treat such conditions contain a TGF-β mimic.