(3S,4R)-4-amino-3-methyl-piperidine-1-carboxylic acid tert-butyl ester | 1290191-72-8

• 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: (3S,4R)-4-amino-3-methyl-piperidine-1-carboxylic acid tert-butyl ester
• 英文别名: cis-racemic-tert-butyl 4-amino-3-methylpiperidine-1-carboxylate；tert-butyl (3S,4R)-4-amino-3-methyl-piperidine-1-carboxylate；cis-4-Amino-3-methyl-1-Boc-piperidine；Tert-butyl cis-4-amino-3-methylpiperidine-1-carboxylate；tert-butyl (3S,4R)-4-amino-3-methylpiperidine-1-carboxylate
• CAS: 1290191-72-8
• 化学式: C₁₁H₂₂N₂O₂
• 分子量: 214.308
• InChiKey: UMBWKSXEVUZEMI-DTWKUNHWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.91
• 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：

  (3S,4R)-4-amino-3-methyl-piperidine-1-carboxylic acid tert-butyl ester 在 三乙酰氧基硼氢化钠 、 溶剂黄146 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 、 1,2-二氯乙烷 、 异丙醇 为溶剂， 反应 1.0h， 生成 (3S,4R)-1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-3-methyl-N-(tetrahydro-2H-pyran-4-yl)piperidin-4-amine
  参考文献：
  名称：

  [EN] KAPPA OPIOID RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO
  [FR] ANTAGONISTES DU RÉCEPTEUR OPIOÏDE KAPPA ET PRODUITS ET PROCÉDÉS ASSOCIÉS

  摘要：

  公开号：

  WO2018170492A9

文献信息

• CONDENSED PYRIDINE COMPOUND
  申请人：Shirakami Shohei

  公开号：US20100105661A1

  公开（公告）日：2010-04-29

  The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention. More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g., cancer and leukemia).

  本发明提供了一种具有出色JAK3抑制活性的化合物，可作为治疗和/或预防各种免疫疾病，包括自身免疫性疾病、炎症性疾病和过敏性疾病的药剂的有效成分。通过对新型紧缩杂环衍生物的研究，发明人已经验证，紧缩吡啶化合物具有出色的JAK3抑制活性，从而完成了本发明。更具体地说，已经验证，由于本发明的化合物具有对JAK3的抑制活性，因此该化合物可用作治疗或预防由不良细胞因子信号转导引起的疾病（例如，在活体器官/组织移植期间的排斥反应、自身免疫性疾病、哮喘、特应性皮炎、风湿病、牛皮癣和动脉粥样硬化疾病），或由异常细胞因子信号转导引起的疾病（例如癌症和白血病）的有效成分。
• 4,6-DIAMINONICOTINAMIDE COMPOUND
  申请人：Shirakami Shohei

  公开号：US20110230467A1

  公开（公告）日：2011-09-22

  [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.

  [问题] 本发明提供了一种4,6-二氨基烟酰胺化合物，该化合物可用作制药组合物的活性成分，特别是用于治疗由不良和/或异常的细胞因子信号传导引起的疾病的制药组合物。 [解决方法] 本发明人广泛研究了具有JAK3抑制作用的化合物，结果发现本发明的4,6-二氨基烟酰胺化合物具有出色的JAK3抑制作用，并且可用作预防或治疗由不良和/或异常的细胞因子信号传导引起的疾病的药剂，从而完成了本发明。
• TRANSAMINASE MUTANT AND USE THEREOF
  申请人：Asymchem Life Science (Tianjin) Co., Ltd.

  公开号：EP3677674A1

  公开（公告）日：2020-07-08

  Disclosed are transaminase mutants and use thereof. The amino acid sequence of the transaminase mutant is obtained by the mutation of the amino acid sequence as shown in SEQ ID NO: 1, and the mutation at least comprises one of the following mutation sites: the 19-th site, the 41-th site, the 43-th site, the 72-th site, the 76-th site, the 92-th site, the 107-th site, the 125-th site, the 132-th site, the 226-th site, the 292-th site, the 295-th site, the 308-th site, and the 332-th site; and the 19-th site is mutated into a serine, the 41-th site is mutated into a serine, the 43-th site is mutated into an asparagine, a glycine in the 72-th site is mutated into a leucine, etc.; or the amino acid sequence of the transaminase mutant has the mutation sites in the mutanted amino acid sequence, and has more than 80% homology to the mutanted amino acid sequence.

  公开了转氨酶突变体及其用途。转氨酶突变体的氨基酸序列是通过突变 SEQ ID NO: 1 所示的氨基酸序列获得的，该突变至少包括以下突变位点中的一个：第 19 位点、第 41 位点、第 43 位点、第 72 位点、第 76 位点、第 92 位点、第 107 位点、第 125 位点、第 132 位点、第 226 位点、第 292 位点、第 295 位点、第 308 位点和第 332 位点；第 19 位点突变为丝氨酸，第 41 位点突变为丝氨酸，第 43 位点突变为天冬酰胺，第 72 位点中的甘氨酸突变为亮氨酸等。或转氨酶突变体的氨基酸序列具有突变氨基酸序列中的突变位点，并且与突变氨基酸序列的同源性超过 80%。
• 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。