CAS: 1129669-05-1; 3-((4-Fluorophenethyl)Amino)-1-Methyl-4-(2-Methyl-1H-Indol-3-yl)-1H-Pyrrole-2,5-Dione

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1-methyl-3-bromo-4-(2-methyl-1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione carbon monoxide 4-fluoro-2-phenethylamine

合成工艺路线路线简述

  • 合成目标产物 Im-12 主要起始原料 1H-Pyrrole-2,5-Dione, 3-Bromo-1-Methyl-4-(2-Methyl-1H-Indol-3-yl)- And 4-Fluorophenethylamine
  • (文献来源)合成步骤主要原料 1H-Pyrrole-2,5-Dione, 3-Bromo-1-Methyl-4-(2-Methyl-1H-Indol-3-yl)- 和 4-Fluorophenethylamine
📜1-Methyl-3-Bromo-4-(2-Methyl-1H-3-Indolyl)-2,5-Dihydro-1H-2,5-Pyrroledione,4-氟苯乙胺置于三乙胺体系中,用 1,4-二氧六环 用作溶剂,以69%的收率获得3-[[2-(4-氟苯基)乙基]氨基]-1-甲基-4-(2-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
参考文献:新型 3-氨基羰基-,3-烷氧基羰基-和 3-氨基-4-吲哚基马来酰亚胺的催化和化学计量合成
标题:新型 3-氨基羰基-,3-烷氧基羰基-和 3-氨基-4-吲哚基马来酰亚胺的催化和化学计量合成
摘要:在碳存在下,通过钯催化的烷氧基和氨基羰基化 3-溴-1-甲基-4-(2-甲基-3-吲哚基)马来酰亚胺(1)与醇和胺,合成了新型的非对称取代的 4-吲哚基马来酰亚胺一氧化氮.由此产生的甲酰胺衍生物代表了一类新的潜在生物活性化合物.此外,1 的直接胺化反应在没有催化剂的情况下顺利进行,并以非常好的收率获得所需的 3-氨基-4-吲哚基马来酰亚胺.(© Wiley-Vch Verlag Gmbh & Co. Kgaa,69451 Weinheim,德国,2009)
Doi:10.1002/ejoc.200800964

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专利信息


专利号:WO-2022121356-A1
优先权日:2020-12-07
标 题:Composition and use thereof in improving anti-tumor effect of vitamin c
发明人：ZHENG HUI; LI CHANGPENG; WANG FUHUI
权利人:GUANGZHOU INST BIOMED & HEALTH
摘要:A composition, comprising an O-GlcNAc glycosyltransferase inhibitor and a glycogen synthesis kinase 3β activator. The O-GlcNAc glycosyltransferase inhibitor is selected from 2-[(4-chlorophenyl) imino] tetrahydro-4-oxo-3-(2-tricyclo [3.3. 1.13, 7] decyl-1-ethyl)-2H-1, 3-thiazin-6-carboxylic acid, and the glycogen synthase kinase 3β activator is selected from 3-[[2-(4-fluorophenyl) ethyl] amino]-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2, 5-dione. The composition has an anti-tumor effect, and can improve the anti-tumor effect of vitamin C. A tumor is selected from colon cancer, rectal cancer, or colorectal cancer.

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主要参考文献


1: Dadarwal D, Mapletoft RJ, Adams GP, Pfeifer LF, Creelman C, Singh J. Effect of progesterone concentration and duration of proestrus on fertility in beef cattle after fixed-time artificial insemination. Theriogenology. 2013 Mar 15;79(5):859-66. doi: 10.1016/j.theriogenology.2013.01.003. doi: 10.1016/j.transproceed.2012.04.034. Epub 2012 Sep 18. doi: 10.1039/c0dt00481b. Epub 2010 Oct 21. doi: 10.1016/j.bmc.2010.07.045. Epub 2010 Jul 25. doi: 10.1152/ajpregu.00336.2009. Epub 2010 Feb 10.
6: GREINER RA, Braathen LR. Cost-effectiveness of biologics for moderate-to-severe psoriasis from the perspective of the Swiss healthcare system. Eur J Dermatol. 2009 Sep-Oct;19(5):494-9. doi: 10.1684/ejd.2009.0725. Epub 2009 Jun 5. doi: 10.1111/j.1468-1331.2009.02663.x. Epub 2009 May 22.
11: Paillaud JL, Harbuzaru B, Patarin J, Bats N. Extra-large-pore zeolites with two-dimensional channels formed by 14 and 12 rings. Science. 2004 May 14;304(5673):990-2. Antenatal corticosteroid therapy for fetal maturation. J Obstet Gynaecol Can. 2003 Jan;25(1):45-52. English, French.

合成参考文献


参考文献:10.1016/j.cell.2004.09.019
摘要:Lu W, Yamamoto V, Ortega B, Baltimore D. Mammalian Ryk is a Wnt coreceptor required for stimulation of neurite outgrowth. Cell. 2004 Oct 01;119(1):97–108. doi: 10.1016/j.cell.2004.09.019.
参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
参考文献:10.2337/diabetes.48.8.1662
摘要:Eldar-Finkelman H, Schreyer SA, Shinohara MM, LeBoeuf RC, Krebs EG. Increased glycogen synthase kinase-3 activity in diabetes- and obesity-prone C57BL/6J mice. Diabetes. 1999 Aug;48(8):1662–6. doi: 10.2337/diabetes.48.8.1662.
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