(4-Aminophenyl) piperidine-1-carboxylate

• 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: (4-Aminophenyl) piperidine-1-carboxylate
• 英文别名: (4-aminophenyl) piperidine-1-carboxylate
• 化学式: C₁₂H₁₆N₂O₂
• 分子量: 220.27
• InChiKey: FKIOEZXXMPKMJB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] PROCESS FOR PREPARING INTERMEDIATE OF ANTI-TUMOR DRUG NIRAPARIB AND INTERMEDIATE THEREOF<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION D'UN INTERMÉDIAIRE POUR LA SYNTHÈSE DU MÉDICAMENT ANTITUMORAL NIRAPARIB ET INTERMÉDIAIRE POUR LA SYNTHÈSE DE CELUI-CI
  申请人：ZAI LAB SHANGHAI CO LTD

  公开号：WO2019072237A1

  公开（公告）日：2019-04-18

  Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound (f), which comprises conducting a cyclization reaction of compound (e) in a solvent and in the presence of a base to give compound (f). The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value.

  本发明公开了一种制备抗肿瘤药物尼拉帕尼布的中间体及其中间体的方法。本发明公开了一种制备化合物（f）的方法，其包括在溶剂和碱的存在下对化合物（e）进行环化反应，从而得到化合物（f）。本发明的方法不涉及贵金属的催化还原或催化偶联反应和手性分离步骤，具有低设备要求、操作简单、有利于工业生产、避免含重金属和磷的废液、成本低、产品ee值高等优点。
• PROCESS FOR PREPARING INTERMEDIATE OF ANTI-TUMOR DRUG NIRAPARIB AND INTERMEDIATE THEREOF
  申请人：Zai Lab (Shanghai) Co., Ltd.

  公开号：EP3694836A1

  公开（公告）日：2020-08-19
• WEE1 INHIBITOR AND PREPARATION AND USE THEREOF
  申请人：SHOUYAO HOLDINGS (BEIJING) CO., LTD.

  公开号：US20220194960A1

  公开（公告）日：2022-06-23

  The present invention relates to a WEE1 inhibitor, and the preparation and use thereof. The WEE1 inhibitor of the present invention is a compound of Formula I or a compound of Formula II, or a pharmaceutically acceptable salt, solvate, polymorph or tautomer thereof. The present invention also provides use of the WEE1 inhibitor in the manufacture of a medicament for the treatment of a disease associated with WEE1 activity. The WEE1 inhibitor provided by the present invention can effectively treat the disease associated with WEE1 activity.