2-(2,4-dimethoxybenzyl)isoindoline-1,3-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 2-(2,4-dimethoxybenzyl)isoindoline-1,3-dione
• 英文别名: 2-[(2,4-dimethoxyphenyl)methyl]isoindole-1,3-dione
• 化学式: C₁₇H₁₅NO₄
• 分子量: 297.31
• InChiKey: ZNIRGYVGIAFTAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  55.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(2,4-dimethoxybenzyl)isoindoline-1,3-dione 在 三溴化硼 作用下， 以 二氯甲烷 为溶剂， 以50 %的产率得到2-(2,4-dihydroxybenzyl)isoindoline-1,3-dione
  参考文献：
  名称：

  Resorcinol-based hemiindigoid derivatives as human tyrosinase inhibitors and melanogenesis suppressors in human melanoma cells

  摘要：

  DOI：

  10.1016/j.ejmech.2022.114972
• 作为产物：
  描述：

  间苯二甲醚 、 O-phthalimidomethyl trichloroacetamidate 在 三氟甲磺酸三甲基硅酯 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以78%的产率得到2-(2,4-dimethoxybenzyl)isoindoline-1,3-dione
  参考文献：
  名称：

  Imidomethylation of C-nucleophiles using O-phthalimidomethyl trichloroacetimidate and catalytic amounts of TMSOTf

  摘要：

  The O-phthalimidomethyl trichloroacetimidate (1), as a latent aminomethylating agent, exhibits high electrophilicity towards a variety of C-nucleophiles in the presence of catalytic amounts of TMSOTf and mild reaction conditions. The nucleophiles include aromatics, alkenes and active methylene compounds 2-11 whereby a phthalimidomethyl group could be introduced to give compounds 12-22. Removal of the phthaloyl group gave the respective amines, beta-amino ketones, and beta-amino acids. The O-(trichloroacetamido)methyl trichloroacetimidate (35) was also found to be a good amidomethylating agent. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2004.04.011

文献信息

• [EN] COMPOSITIONS FOR PROMOTING READTHROUGH OF PREMATURE TERMINATION CODONS, AND METHODS OF USING THE SAME<br/>[FR] COMPOSITIONS PERMETTANT DE FAVORISER LA TRANSLECTURE DE CODONS DE TERMINAISON PRÉMATURÉE, ET LEURS PROCÉDÉS D'UTILISATION
  申请人：THE CENTRE FOR DRUG RES AND DEV

  公开号：WO2017049409A1

  公开（公告）日：2017-03-30

  Disclosed are compounds of general formula (I) that promote readthrough of a premature termination codon (PTC) of an RNA molecule in a translation system, and their use, alone or in combination with other compounds, such as aminoglycoside, to treat diseases or disorders ameliorated by modulation of a premature termination codon (PTC) of an RNA molecule in a translation system. The disorder or disease may be Dystrophic epidermolysis bullosa, Batten disease, Duchenne muscular dystrophy, cancer, and spinal muscular atrophy. Ar-L-B (I)

  公开了通式(I)的化合物，它们能够促进RNA分子在翻译系统中过早终止密码子(PTC)的通读，以及它们单独或与其他化合物如氨基糖苷的组合使用，用于治疗通过调节翻译系统中RNA分子的过早终止密码子(PTC)而得到改善的疾病或失调。该疾病或失调可能是营养不良性表皮松解症、贝敦病、杜氏肌营养不良症、癌症和脊髓性肌萎缩症。Ar-L-B (I)
• [EN] INHIBITORS OF IRES-MEDIATED PROTEIN SYNTHESIS<br/>[FR] INHIBITEURS DE SYNTHÈSE DE PROTÉINES MÉDIÉE PAR DES IRES
  申请人：UNIV CALIFORNIA

  公开号：WO2017192665A1

  公开（公告）日：2017-11-09

  This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

  本公开涉及IRES介导的蛋白质合成抑制剂，包含这些化合物的治疗有效量的组合物，以及使用这些化合物和组合物治疗过度增殖性疾病（例如癌症）的方法。本公开还涉及包含IRES介导的蛋白质合成抑制剂和mTOR抑制剂的组合物，以及通过联合给药IRES介导的蛋白质合成抑制剂和mTOR抑制剂治疗癌症的方法。
• INHIBITORS OF IRES-MEDIATED PROTEIN SYNTHESIS
  申请人：The Regents of the University of California

  公开号：EP3452447A1

  公开（公告）日：2019-03-13
• JPH0625163A
  申请人：——

  公开号：JPH0625163A

  公开（公告）日：1994-02-01
• Imidomethylation of C-nucleophiles using O-phthalimidomethyl trichloroacetimidate and catalytic amounts of TMSOTf
  作者：Ibrahim A.I Ali、El Sayed H El Ashry、Richard R Schmidt

  DOI：10.1016/j.tet.2004.04.011

  日期：2004.5

  The O-phthalimidomethyl trichloroacetimidate (1), as a latent aminomethylating agent, exhibits high electrophilicity towards a variety of C-nucleophiles in the presence of catalytic amounts of TMSOTf and mild reaction conditions. The nucleophiles include aromatics, alkenes and active methylene compounds 2-11 whereby a phthalimidomethyl group could be introduced to give compounds 12-22. Removal of the phthaloyl group gave the respective amines, beta-amino ketones, and beta-amino acids. The O-(trichloroacetamido)methyl trichloroacetimidate (35) was also found to be a good amidomethylating agent. (C) 2004 Elsevier Ltd. All rights reserved.