tert-butyl 2-(piperidin-4-yl)acetate hydrochloride | 2174007-91-9

• 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: tert-butyl 2-(piperidin-4-yl)acetate hydrochloride
• 英文别名: tert-butyl 2-(4-piperidyl)acetate hydrochloride；tert-butyl 2-piperidin-4-ylacetate;hydrochloride
• CAS: 2174007-91-9
• 化学式: C₁₁H₂₁NO₂*ClH
• 分子量: 235.754
• InChiKey: AXNZZFDNHDADAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.14
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  38.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tert-butyl 2-(piperidin-4-yl)acetate hydrochloride 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 palladium 10% on activated carbon 、 氢气 、 caesium carbonate 、 N,N-二异丙基乙胺 作用下， 以 1,4-二氧六环 、 水 、 二甲基亚砜 、 乙酸乙酯 为溶剂， 反应 36.0h， 生成 tert-butyl 2-[1-[5-(2,6-dioxo-3-piperidyl)-3-fluoro-2-pyridyl]-4-piperidyl]acetate
  参考文献：
  名称：

  [EN] COMPOUNDS FOR TARGETING DEGRADATION OF IRAK4 PROTEINS
  [FR] COMPOSÉS POUR LE CIBLAGE DE LA DÉGRADATION DE PROTÉINES IRAK4

  摘要：

  This disclosure relates to compounds of Formula (A): IRAK—L—DSM (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.

  公开号：

  WO2023283610A1
• 作为产物：
  描述：

  1,1-dimethylethyl 4-[(1,1-dimethylethyloxycarbonyl)methyl]-1-piperidinecarboxylate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 以72.39 %的产率得到tert-butyl 2-(piperidin-4-yl)acetate hydrochloride
  参考文献：
  名称：

  [EN] COMPOUNDS FOR TARGETING DEGRADATION OF IRAK4 PROTEINS
  [FR] COMPOSÉS POUR LE CIBLAGE DE LA DÉGRADATION DE PROTÉINES IRAK4

  摘要：

  This disclosure relates to compounds of Formula (A): IRAK—L—DSM (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.

  公开号：

  WO2023283610A1

文献信息

• [EN] BICYCLIC-SUBSTITUTED GLUTARIMIDE CEREBLON BINDERS<br/>[FR] LIANTS DE CÉRÉBLON DE GLUTARIMIDE À SUBSTITUTION BICYCLIQUE
  申请人：C4 THERAPEUTICS INC

  公开号：WO2023239750A1

  公开（公告）日：2023-12-14

  This invention provides Degron compounds which bind to cereblon which is a component of the E3 ubiquitin ligase. The Degrons provided herein can be used to modulate the activity of cereblon either alone or as covalently linked to a Tail. Alternatively, the Degron can be linked to a Targeting Ligand which binds to a Target Protein for protein degradation.

  本发明提供与脑龙结合的 Degron 化合物，脑龙是 E3 泛素连接酶的一个组成部分。本发明提供的 Degron 可单独用于调节大脑龙的活性，也可与尾部共价连接。另外，Degron 还可以与靶向配体连接，靶向配体可与靶蛋白结合进行蛋白降解。
• [EN] BIFUNCTIONAL DEGRADERS OF HEMATOPOIETIC PROGENITOR KINASE AND THERAPEUTIC USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION BIFONCTIONNELS DE PROGÉNITEUR HÉMATOPOÏÉTIQUE KINASE ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：[en]NURIX THERAPEUTICS, INC.

  公开号：WO2023086399A1

  公开（公告）日：2023-05-19

  The present disclosure provides bifunctional compounds as HPK1 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by HPK1.