6-maleimido-3-oxahexanoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 6-maleimido-3-oxahexanoic acid
• 英文别名: 2-[3-(2,5-Dioxopyrrol-1-yl)propoxy]acetic acid；2-[3-(2,5-dioxopyrrol-1-yl)propoxy]acetic acid
• 化学式: C₉H₁₁NO₅
• 分子量: 213.19
• InChiKey: PCTFNRHBQVOWGC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  83.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  6-maleimido-3-oxahexanoic acid 、 多西他赛 在 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以612 mg的产率得到2'-(6-maleimido-3-oxa-hexanoyl)-docetaxel
  参考文献：
  名称：

  CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION

  摘要：

  本发明涉及一种羟烷基淀粉共轭物及其制备方法，所述羟烷基淀粉共轭物包括羟烷基淀粉衍生物和细胞毒性药剂，所述细胞毒性药剂包括至少一个次级羟基，其中羟烷基淀粉通过所述次级羟基与细胞毒性药剂连接。根据本发明的共轭物具有以下公式HAS'(-L-M)n的结构，其中M是细胞毒性药剂的残基，L是连接基团，HAS'是羟烷基淀粉衍生物的残基，n大于或等于1，且羟烷基淀粉衍生物的平均分子量（MW）高于肾脏阈值。

  公开号：

  US20150297738A1
• 作为产物：
  描述：

  N-甲氧基羰基顺丁烯二酰亚胺 、 6-amino-3-oxahexanoic acid trifluoroacetate 在 碳酸氢钠 作用下， 以 水 为溶剂， 反应 3.5h， 生成 6-maleimido-3-oxahexanoic acid
  参考文献：
  名称：

  CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION

  摘要：

  本发明涉及一种羟烷基淀粉共轭物及其制备方法，所述羟烷基淀粉共轭物包括羟烷基淀粉衍生物和细胞毒性药剂，所述细胞毒性药剂包括至少一个次级羟基，其中羟烷基淀粉通过所述次级羟基与细胞毒性药剂连接。根据本发明的共轭物具有以下公式HAS'(-L-M)n的结构，其中M是细胞毒性药剂的残基，L是连接基团，HAS'是羟烷基淀粉衍生物的残基，n大于或等于1，且羟烷基淀粉衍生物的平均分子量（MW）高于肾脏阈值。

  公开号：

  US20150297738A1

文献信息

• [EN] CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION<br/>[FR] CONJUGUÉS COMPRENANT DE L'HYDROXYALKYLAMIDON ET UN AGENT CYTOTOXIQUE ET LEUR PROCÉDÉ DE SYNTHÈSE
  申请人：FRESENIUS KABI DE GMBH

  公开号：WO2012004005A1

  公开（公告）日：2012-01-12

  The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS'(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS' is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.
• [EN] CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION<br/>[FR] CONJUGUÉS COMPRENANT UN AMIDON HYDROXYALKYLÉ ET UN AGENT CYTOTOXIQUE ET LEUR PROCÉDÉ DE PRÉPARATION
  申请人：FRESENIUS KABI DE GMBH

  公开号：WO2012004006A1

  公开（公告）日：2012-01-12

  The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS'(-L-M)n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS' is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.
• CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION
  申请人：Fresenius Kabi Deutschland GmbH

  公开号：US20150297738A1

  公开（公告）日：2015-10-22

  The present invention relates to a hydroxyalkyl starch conjugate and a method for preparing the same, said hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one secondary hydroxyl group, wherein the hydroxyalkyl starch is linked via said secondary hydroxyl group to the cytotoxic agent. The conjugate according to the present invention has a structure according to the following formula HAS′(-L-M) n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS′ is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold.

  本发明涉及一种羟烷基淀粉共轭物及其制备方法，所述羟烷基淀粉共轭物包括羟烷基淀粉衍生物和细胞毒性药剂，所述细胞毒性药剂包括至少一个次级羟基，其中羟烷基淀粉通过所述次级羟基与细胞毒性药剂连接。根据本发明的共轭物具有以下公式HAS'(-L-M)n的结构，其中M是细胞毒性药剂的残基，L是连接基团，HAS'是羟烷基淀粉衍生物的残基，n大于或等于1，且羟烷基淀粉衍生物的平均分子量（MW）高于肾脏阈值。