CAS: 22013-33-8; 2,3-Dihydrobenzo[b][1,4]Dioxin-6-Amine

该化合物是一种该化合物是一种苯并二恶英核心,在六点方位有一个地雷功能组,这种结构在合成应用中具有多功能性,特别是作为制药和农用化学的关键中间体,其硬性苯并二恶英剑片可增强稳定性,而该矿组则允许进一步发挥功能,使其在生物活性分子的开发中具有价值.复合物在普通有机溶剂中表现出有利的溶解性,便于在多种反应条件下使用.其定义明确的再活性特征和与标准合成方法的兼容性强调了其在药用化学和材料科学研究中的实用性.

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上下游产品

CAS号16498-20-7 3,4-亚乙基二氧硝基苯 | CAS号493-09-4 1,4-苯并二噁烷 | CAS号62140-78-7 7-硝基-2,3-二氢-苯并[... | CAS号52287-51-1 6-溴-1,4-苯并二恶烷 | CAS号120-80-9 邻苯二酚 | CAS号57744-67-9 6-碘-1,4-苯并二氧烷 | CAS号52791-05-6 4-氯-6,7-二亚甲基二羟喹唑啉 | CAS号148245-18-5 哌嗪,1-(2,3-二氢-1,... | CAS号42477-07-6 2-氯-N-(2,3-二氢苯并... | CAS号30211-36-0 9-methyl-2,3-di... | CAS号81864-47-3 6,7-二氢-1H-[1,4]... | CAS号128650-18-0 5H-(2)benzopyra... | CAS号100254-21-5 N-(2,3-二氢苯并[b][... | CAS号10288-72-9 6-羟基-1,4-苯并二噁烷 | CAS号100275-94-3 6-异氰酸基-1,4-苯并二噁烷

合成工艺路线路线简述

    📜6-溴-1,4-苯并恶烷置于4,4'-二甲基-2,2'-联吡啶,碳酸氢铵,Nickel Diacetate,1,8-二氮杂双环[5.4.0]十一碳-7-烯,Potassium Bromide体系中,用 四氢呋喃,N,N-二甲基乙酰胺 用作溶剂,以75 %的收率获得6-氨基-1,4-苯并二氧杂环
    参考文献:Ni 催化芳基卤化物与铵盐偶联光化学合成苯胺
    标题:Ni 催化芳基卤化物与铵盐偶联光化学合成苯胺
    摘要:简单,高效和经济地合成苯胺仍然是合成化学中的一个重要挑战.在这项研究中,Ni(Oac) 2-联吡啶络合物表明在光的直接激发下很容易催化芳基卤化物与铵盐的胺化反应,从而使多种芳基氯和溴转化为相应的伯(杂) 在没有外部光敏剂的情况下的芳基胺.药物分子的后期修饰和伯芳基胺的15 N-标记也通过许多示例进行了演示.光诱导产生 Ni(I)-联吡啶物种被认为是反应中的关键步骤,使 Ni(I)/ni(III) 循环能够进行催化转换.
    Doi:10.1021/acscatal.2C04959

    海关参考信息

    专利信息


    专利号:US-5342947-A
    优先权日:1992-10-09
    标 题:Preparation of water soluble camptothecin derivatives
    发明人:LACKEY Karen; STERNBACH DANIEL D
    权利人:GLAXO INC
    摘要:The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), (I) wherein: n represents the integer 1 or 2; R1 represents independently, hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; and R2 represents hydrogen and the pharmaceutically acceptable salts thereof.

    专利号:US-6849650-B2
    优先权日:1998-02-27
    标 题:Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
    发明人:THORSETT EUGENE D; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES
    权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:US-6399628-B1
    优先权日:1996-11-22
    标 题 :N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds
    发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; REEL JON K; THORSETT EUGENE D; WHITESITT CELIA A
    权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:EP-0951466-B1
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
    发明人:WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D
    权利人:ELAN PHARM INC; LILLY CO ELI
    摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:US-7390801-B2
    优先权日:1996-12-23
    标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
    发明人:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J
    权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

    专利号:US-7632972-B2
    优先权日:2003-10-30
    标 题 :Compounds and methods for treatment of cancer and modulation of programmed cell death for melanoma and other cancer cells
    发明人:HERGENROTHER PAUL J; NESTERENKO VITALIY; PUTT KARSON; ALLEN BRITTANY JOY; DOTHAGER ROBIN SHANE; LESLIE BENJAMIN JAMES
    权利人:UNIV ALABAMA
    摘要:Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    [参考文献]: Ajay Kumar, Et Al. Synthesis Of Novel Functionalized 4-Aza-2,3-Didehydropodophyllotoxin Derivatives With Potential Antitumor Activity. J Heterocycl Chem. 2010 Nov;47(6):1275-1282.

    合成参考文献


    摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 123.
    摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 120.
    摘要:Xi, C.; Chen, C., Science of Synthesis: Multicomponent Reactions, (2013) 2, 444.
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