(2S)-2-amino-1-piperidinecarboxylic acid 1,1-dimethylethyl ester

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (2S)-2-amino-1-piperidinecarboxylic acid 1,1-dimethylethyl ester
• 英文别名: 1,1-dimethylethyl (2S)-2-amino-1-piperidinecarboxylate；S-amino-1-Boc-piperidine；tert-butyl (2S)-2-aminopiperidine-1-carboxylate
• 化学式: C₁₀H₂₀N₂O₂
• 分子量: 200.281
• InChiKey: GEHBIWVQKQLYNB-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (4aR,10bS)-1-[(5-fluoroimidazo[1,2-a]pyridin-2-yl)methyl]-1,2,3,4,4a,5,6,10b-octahydro-1,10-phenanthroline 、 (2S)-2-amino-1-piperidinecarboxylic acid 1,1-dimethylethyl ester 在 乙腈 、 水 、 三氟乙酸 作用下， 以 乙醇 为溶剂， 反应 6.0h， 以to afford 1,1-dimethylethyl (2S)-2-({2-[(4aR,10bS)-3,4,4a,5,6,10b-hexahydro-1,10-phenanthrolin-1(2H)-ylmethyl]imidazo[1,2-a]pyridin-5-yl}amino)-1-piperidinecarboxylate which的产率得到1,1-dimethylethyl (2S)-2-({2-[(4aR,10bS)-3,4,4a,5,6,10b-hexahydro-1,10-phenanthrolin-1(2H)-ylmethyl]imidazo[1,2-a]pyridin-5-yl}amino)-1-piperidinecarboxylate
  参考文献：
  名称：

  Chemical Compounds

  摘要：

  本发明提供了式（I）的化合物，包括盐、溶剂化合物和生理功能衍生物，以及含有它们的制药配方、它们的制备过程和使用它们的治疗方法。

  公开号：

  US20090093454A1

文献信息

• [EN] THERAPEUTIC OXY-PHENYL-ARYL COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS OXY-PHÉNYL-ARYLES THÉRAPEUTIQUES ET LEUR UTILISATION
  申请人：CANCER REC TECH LTD

  公开号：WO2009053694A1

  公开（公告）日：2009-04-30

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

  本发明总体涉及治疗化合物领域，更具体地涉及如本文所述的某些氧基苯基芳基化合物（以下简称OPA化合物），其中，抑制检查点激酶2（CHK2）激酶功能。本发明还涉及包含此类化合物的药物组合物，以及使用此类化合物和组合物，在体内外抑制CHK2激酶功能，以及治疗由CHK2介导的疾病和状况，包括通过抑制CHK2激酶功能而改善的疾病和状况，等等，包括诸如癌症等增殖性疾病，可选地与另一剂联合使用，例如，（a）DNA拓扑异构酶I或II抑制剂；（b）DNA损伤剂；（c）抗代谢物或TS抑制剂；（d）针对微管的药剂；（e）电离辐射。
• TRANSAMINASE MUTANT AND APPLICATION THEREOF
  申请人：Asymchem Life Science (Tianjin) Co., Ltd

  公开号：EP3733689A1

  公开（公告）日：2020-11-04

  The invention provides a transaminase mutant and application thereof, wherein the amino acid sequence of the transaminase mutant is formed after mutation of the amino acid sequence as shown in SEQ ID NO: 1, and mutated amino acid sites comprise T7C+S47C sites. The transaminase mutant having the mutation sites can be further prepared into an immobilized enzyme through an immobilization technology, the immobilized enzyme has relatively high activity and high stability, can be recycled for multiple times, and is applicable to continuous flow reaction in a packed bed.

  本发明提供了一种转氨酶突变体及其应用，其中转氨酶突变体的氨基酸序列是由SEQ ID NO: 1所示氨基酸序列突变后形成的，突变氨基酸位点包括T7C+S47C位点。具有突变位点的转氨酶突变体可通过固定化技术进一步制备成固定化酶，该固定化酶具有较高的活性和较高的稳定性，可多次循环使用，适用于填料床连续流反应。
• Transaminase mutant and application thereof
  申请人：ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD

  公开号：US11359219B2

  公开（公告）日：2022-06-14

  The invention provides a transaminase mutant and application thereof, wherein the amino acid sequence of the transaminase mutant is formed after mutation of the amino acid sequence as shown in SEQ ID NO: 1, and mutated amino acid sites comprise T7C+S47C sites. The transaminase mutant having the mutation sites can be further prepared into an immobilized enzyme through an immobilization technology, the immobilized enzyme has relatively high activity and high stability, can be recycled for multiple times, and is applicable to continuous flow reaction in a packed bed.

  本发明提供了一种转氨酶突变体及其应用，其中转氨酶突变体的氨基酸序列是由SEQ ID NO: 1所示氨基酸序列突变后形成的，突变氨基酸位点包括T7C+S47C位点。具有突变位点的转氨酶突变体可以通过固定化技术进一步制备成固定化酶，固定化酶具有较高的活性和较高的稳定性，可以多次循环使用，适用于填料床连续流反应。
• THERAPEUTIC OXY-PHENYL-ARYL COMPOUNDS AND THEIR USE
  申请人：Cancer Research Technology Limited

  公开号：EP2227460A1

  公开（公告）日：2010-09-15
• CN117186097
  申请人：——

  公开号：——

  公开（公告）日：——