Boc-Lys(H)(Ox)-OMe | 1042975-32-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: Boc-Lys(H)(Ox)-OMe
• CAS: 1042975-32-5
• 化学式: C₁₅H₂₅N₃O₅
• 分子量: 327.381
• InChiKey: XZVNTFWYBCASRN-JTQLQIEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
  None
• 可旋转键数：
  None
• 环数：
  None
• sp3杂化的碳原子比例：
  None
• 拓扑面积：
  None
• 氢给体数：
  None
• 氢受体数：
  None

反应信息

• 作为反应物：
  描述：

  Boc-Lys(H)(Ox)-OMe 、 氯甲酸烯丙酯 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 15.0h， 以100%的产率得到methyl (S)-2-(2,2-dimethyl-4,12-dioxo-3,13-dioxa-5,11-diazahexadec-15-en-6-yl)oxazole-4-carboxylate
  参考文献：
  名称：

  Cyclooligomerization of a Helix-Bearing Template into Macrocycles Bearing Multiple Helices

  摘要：

  Cyclooligomerization was investigated for separating and spatially arranging helical peptides as discontinuous surfaces. Tetrapeptide H-[Ile-Ser-Lys(Ox)]-OH, containing a turn-inducing oxazole constraint, was connected through its lysine side chain via a beta-alanine linker to the C-terminus of a two-turn helical nonapeptide Ac-(cyclo-4,8)-LRL [KARAD](Aib). The resulting helix-appended template was self-condensed and cyclized to a library of macrocycles (n = 2-6) containing multiple (2-6) helices. An NMR structure shows retention of alpha helicity in the cyclotrimer (n = 3).

  DOI：

  10.1021/ol801040c
• 作为产物：
  描述：

  Boc-Lys(Cbz)(Ox)-OMe 在 10% Pd on charcoal 、 氢气 作用下， 以 甲醇 、 乙酸乙酯 为溶剂， 20.0 ℃ 、241.32 kPa 条件下， 以100%的产率得到Boc-Lys(H)(Ox)-OMe
  参考文献：
  名称：

  Cyclooligomerization of a Helix-Bearing Template into Macrocycles Bearing Multiple Helices

  摘要：

  Cyclooligomerization was investigated for separating and spatially arranging helical peptides as discontinuous surfaces. Tetrapeptide H-[Ile-Ser-Lys(Ox)]-OH, containing a turn-inducing oxazole constraint, was connected through its lysine side chain via a beta-alanine linker to the C-terminus of a two-turn helical nonapeptide Ac-(cyclo-4,8)-LRL [KARAD](Aib). The resulting helix-appended template was self-condensed and cyclized to a library of macrocycles (n = 2-6) containing multiple (2-6) helices. An NMR structure shows retention of alpha helicity in the cyclotrimer (n = 3).

  DOI：

  10.1021/ol801040c

文献信息

• [EN] METHODS OF MAKING INCRETIN ANALOGS<br/>[FR] PROCÉDÉS DE FABRICATION D'ANALOGUES D'INCRÉTINE
  申请人：LILLY CO ELI

  公开号：WO2021034815A1

  公开（公告）日：2021-02-25

  Intermediate compounds are disclosed for making incretin analogs, or pharmaceutically acceptable salts thereof. In addition, methods are disclosed for making incretin analogs by coupling from two to four of the intermediate compounds herein via hybrid liquid solid phase synthesis or native chemical ligation.

  本发明公开了制备胰高血糖素类似物或其药用可接受盐的中间化合物。此外，本发明还公开了通过混合液固相合成或天然化学连接法，通过将本文中的两到四种中间化合物耦合制备胰高血糖素类似物的方法。
• PRODRUGS COMPRISING AN INSULIN LINKER CONJUGATE
  申请人：SANOFI-AVENTIS DEUTSCHLAND GMBH

  公开号：US20150258207A1

  公开（公告）日：2015-09-17

  The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L, wherein D represents the insulin moiety; and -L is a non-biologically active linker moiety -L 1 represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.

  本发明涉及一种前药或其药用可接受的盐，包括胰岛素连接物D-L，其中D代表胰岛素部分；-L是一种非生物活性的连接物-L1，其由式(I)表示，虚线表示通过形成酰胺键与胰岛素的氨基团之一结合。该发明还涉及包括所述前药的药物组合物，以及它们作为治疗或预防可以通过胰岛素治疗的疾病或紊乱的药物的用途。