Bipiperidinyl carboxylic acid

• 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: Bipiperidinyl carboxylic acid
• 英文别名: 1-piperidin-1-ylpiperidine-2-carboxylic acid
• 化学式: C₁₁H₂₀N₂O₂
• 分子量: 212.29
• InChiKey: YNOQFRPIURNTSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Method for the synthesis of irinotecan
  申请人：Synbias Pharma AG

  公开号：EP2881396A1

  公开（公告）日：2015-06-10

  The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin. The present invention is further directed to a method for the synthesis of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) which is used as an intermediate in the synthesis of irinotecan.

  本发明涉及一种合成7-乙基-10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱（即伊立替康）的方法，包括：（a）制备10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱；和（b）选择性地在步骤（a）中的化合物的7位进行乙基化，从而制备出7-乙基-10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱。本发明还涉及一种合成10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱（即7-去乙基伊立替康）的方法，该方法用作合成伊立替康的中间体。
• [EN] METHOD FOR THE SYNTHESIS OF IRINOTECAN<br/>[FR] PROCÉDÉ DE SYNTHÈSE D'IRINOTÉCAN
  申请人：SYNBIAS PHARMA AG

  公开号：WO2015082240A1

  公开（公告）日：2015-06-11

  The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.

  本发明涉及一种合成7-乙基-10-[4-(1-哌啶基)-1-哌啶基]羰氧基-喜树碱（即伊立替康）的方法，包括：(a)制备10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱；(b)在步骤(a)中选择性地对化合物进行7位乙基化，从而制备7-乙基-10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱。本发明还涉及使用10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱（即7-脱乙基伊立替康）作为合成伊立替康的中间体的方法。
• METHOD FOR THE SYNTHESIS OF IRINOTECAN
  申请人：SYNBIAS PHARMA AG

  公开号：US20160264590A1

  公开（公告）日：2016-09-15

  The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.

  本发明涉及一种合成7-乙基-10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱（即伊立替康）的方法，包括：（a）制备10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱；和（b）选择性地在步骤（a）中的化合物的7位进行乙基化，从而导致制备7-乙基-10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱。本发明还进一步涉及将10-[4-(1-哌啶基)-1-哌啶基]羰氧基喜树碱（即7-去乙基伊立替康）用作合成伊立替康的方法中的中间体。
• EP3030567A1
  申请人：——

  公开号：EP3030567A1

  公开（公告）日：2016-06-15
• US9765083B2
  申请人：——

  公开号：US9765083B2

  公开（公告）日：2017-09-19