diethyl 2-ethyl-3-methylmaleate

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: diethyl 2-ethyl-3-methylmaleate
• 英文别名: diethyl (Z)-2-ethyl-3-methylbut-2-enedioate
• 化学式: C₁₁H₁₈O₄
• 分子量: 214.262
• InChiKey: RDNWVMUUEDXVNS-HJWRWDBZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  52.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  diethyl 2-ethyl-3-methylmaleate 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 反应 0.5h， 以83.7%的产率得到3-乙基-4-甲基呋喃-2,5-二酮
  参考文献：
  名称：

  [EN] SUBSTITUTED AZOLE DIONE COMPOUNDS WITH ANTIVIRAL ACTIVITY
  [FR] COMPOSÉS AZOLE DIONE SUBSTITUÉS À ACTIVITÉ ANTIVIRALE

  摘要：

  本文提供了使用替代咪唑二酮化合物治疗病毒感染的方法。

  公开号：

  WO2021194954A1
• 作为产物：
  描述：

  丙酮酸乙酯 、 ethyl 2-(dimethoxyphosphoryl)butanoate 在 sodium hydride 作用下， 以 乙二醇二甲醚 为溶剂， 以87.2%的产率得到diethyl 2-ethyl-3-methylmaleate
  参考文献：
  名称：

  [EN] SUBSTITUTED AZOLE DIONE COMPOUNDS WITH ANTIVIRAL ACTIVITY
  [FR] COMPOSÉS AZOLE DIONE SUBSTITUÉS À ACTIVITÉ ANTIVIRALE

  摘要：

  本文提供了使用替代咪唑二酮化合物治疗病毒感染的方法。

  公开号：

  WO2021194954A1

文献信息

• Compounds with anti-cancer activity
  申请人：Kawabe Takumi

  公开号：US20080275057A1

  公开（公告）日：2008-11-06

  Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.

  提供了一种新型的取代咪唑二酮，可以杀死细胞，抑制细胞增殖，抑制细胞生长，废除细胞周期G2检查点和/或导致对G2细胞周期阻滞的适应。提供了制备和使用该发明化合物的方法。该发明提供了取代咪唑二酮来治疗细胞增殖紊乱。该发明包括使用取代咪唑二酮来选择性地杀死或抑制癌细胞，而无需额外的抗癌治疗。该发明包括使用细胞周期G2检查点废除的取代咪唑二酮来选择性地使癌细胞对DNA损伤试剂、治疗和/或其他类型的抗癌试剂产生敏感性。
• 2-Ethyl-3-methylmaleimide in Tokyo Bay Sediments Providing the First Evidence for its Formation from Chlorophylls in the Present Photic and Oxygenic Zone
  作者：Masaki KOZONO、Shinya NOMOTO、Hajime MITA、Ryoshi ISHIWATARI、Akira SHIMOYAMA

  DOI：10.1271/bbb.66.1844

  日期：2002.1

  Tokyo Bay bottom sediments were analyzed for 2-ethyl-3-methylmaleimide, a degradation product of chlorophylls, which has been detected in ancient sediments. It was found in all sediments examined in concentrations of about 1 to 15 nmol/g- of dried sediment, and it was shown to be preserved for 100 years in the sediments. Its depth distribution agreed with that of the reported total organic carbon content of the sediments, reflecting a change in primary productivity. We concluded that this maleimide was produced under photic and oxygenic conditions in nature before the incorporation of photosynthesizing organisms into sediments.

  对东京湾海底沉积物中的 2-乙基-3-甲基马来酰亚胺进行了分析，这是一种叶绿素的降解产物，曾在古代沉积物中检测到过。在所有检测的沉积物中都发现了这种物质，其浓度约为 1 至 15 nmol/g-（干燥沉积物），而且在沉积物中可保存 100 年之久。它的深度分布与报告的沉积物总有机碳含量的深度分布一致，反映了初级生产力的变化。我们的结论是，这种马来酰亚胺是在光合作用生物进入沉积物之前，在自然界的光氧条件下产生的。
• COMPOUNDS WITH ANTI-CANCER ACTIVITY
  申请人：KAWABE TAKUMI

  公开号：US20110092514A1

  公开（公告）日：2011-04-21

  Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.

  本发明提供了一种替代的咪唑二酮，可以杀死细胞、抑制细胞增殖、抑制细胞生长、废除细胞周期G2检查点和/或导致适应G2细胞周期停滞。本发明提供了制备和使用该发明化合物的方法。该发明提供了替代的咪唑二酮来治疗细胞增殖障碍。该发明包括使用替代的咪唑二酮选择性地杀死或抑制癌细胞，而不需要额外的抗癌治疗。该发明包括使用细胞周期G2检查点废除的替代的咪唑二酮，以选择性地使癌细胞对DNA损伤试剂、治疗和/或其他类型的抗癌试剂敏感。
• COMPOUNDS THAT ABROGATE THE CELL CYCLE G2 CHECKPOINT FOR USE IN THE TREATMENT OF CANCER
  申请人：CanBas Co., Ltd.

  公开号：EP3088397A1

  公开（公告）日：2016-11-02

  Substituted azole diones (II) and (III) are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making the invention compounds are provided. The invention provides substituted azole diones (II) and (III) to treat cell proliferation disorders. The invention includes the substituted azole diones (II) and (III) for use to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the cell cycle G2- checkpoint-abrogating substituted azole diones (II) and (III) for use to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.

  本发明提供的取代唑二酮类化合物(II)和(III)可杀死细胞、抑制细胞增殖、抑制细胞生长、减弱细胞周期 G2 检查点和/或导致适应 G2 细胞周期停滞。提供了制造本发明化合物的方法。本发明提供了用于治疗细胞增殖障碍的取代唑二酮类化合物（II）和（III）。本发明包括取代的唑二酮(II)和(III)，用于选择性地杀死或抑制癌细胞，而无需额外的抗癌治疗。本发明包括细胞周期G2-检查点消减取代的唑二酮(II)和(III)，用于选择性地使癌细胞对DNA损伤试剂、治疗和/或其它类型的抗癌试剂敏感。
• N-SUBSTITUTED 2,5-DIOXO-AZOLINE COMPOUNDS FOR USE IN THE TREATMENT OF CANCER
  申请人：CanBas Co., Ltd.

  公开号：EP3567035A1

  公开（公告）日：2019-11-13

  Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.

  本发明提供了新型取代唑二酮类化合物，可杀死细胞、抑制细胞增殖、抑制细胞生长、减弱细胞周期 G2 检查点和/或导致细胞周期 G2 停滞。本发明还提供了制造和使用本发明化合物的方法。本发明提供了用于治疗细胞增殖障碍的取代唑二酮类化合物。本发明包括使用取代的唑二酮选择性地杀死或抑制癌细胞，而无需额外的抗癌治疗。本发明包括使用细胞周期G2-检查点抑制取代的唑二酮类化合物选择性地使癌细胞对DNA损伤试剂、治疗和/或其它类型的抗癌试剂敏感。