CAS: 2373-80-0; 3-(Benzo[d][1,3]Dioxol-5-yl)Acrylic Acid

该化合物是有机化合物,其特征为二亚甲基二氧基组,附于一个恶性酸结构,该化合物一般显示白色到白晶状,以潜在生物活动闻名,包括抗氧化剂和抗氟性能,这在制药和化妆应用中引起了兴趣;亚甲二氧基组增强了其再活性,并可能影响其与生物目标的相互作用;就溶解性而言,该化合物一般可溶于有机溶剂,但在水中溶解性可能有限;该化合物的稳定性可能受到光和热的影响,需要谨慎的储存条件;此外,其分子结构允许各种功能性改变,使其成为有机合成的多功能建筑块.

结构式图片

欧盟法规

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上下游产品

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合成工艺路线路线简述

  • 合成目标产物 3,4-(Methylenedioxy)Cinnamic Acid 主要起始原料 (E)-Methyl 3-(Benzo[d][1,3]Dioxol-5-yl)Acrylate
  • (文献来源)合成步骤主要原料 (E)-Methyl 3-(Benzo[d][1,3]Dioxol-5-yl)Acrylate
3,4-(亚甲二氧基)苯亚甲基丙酮置于sodium Hypochlorite,Sodium Hydroxide体系中,用 四氢呋喃,水 用作溶剂,化学反应 0.5H,以60%的收率获得3,4-(亚甲二氧)肉桂酸
参考文献:来自 Hydrocotyle Bonariensis 的二苄基丁内酯木脂素的简化衍生物作为抗锥虫候选物
标题:来自 Hydrocotyle Bonariensis 的二苄基丁内酯木脂素的简化衍生物作为抗锥虫候选物
摘要:寻找生物活性化合物的药效团对药物发现研究至关重要,涉及分子中不同原子的适当排列.作为旨在发现针对原生动物寄生虫克氏锥虫的新候选药物的持续工作的一部分,Hydroctyle Bonariensis的己烷提取物经过生物活性引导分馏,以提供两种化学相关的二苄基丁内酯木脂素-Hinokinin ( 1 ) 和 Hibalactone ( 2 ) . 化合物1和2显示出针对锥鞭毛体的活性,Ec 50值分别为 17.0 和 69.4 μm.化合物1对临床相关形式的寄生虫无鞭毛体也有活性,Ec 50值为 34.4 μm.构效关系(sar)表明c-7处双键的缺失是抗寄生虫活性增加的关键特征.在锥虫中研究了最有效的化合物1的致死作用.Sytox Green 基于荧光的检测表明寄生虫的质膜通透性发生了显着变化.此外,化合物1在 200 μm 时对小鼠红细胞没有显着的溶血活性.为了搜索药效团,三种不同的简化化合物
Doi:10.1002/cbdv.202100515

海关参考信息

专利信息


专利号:US-2003092064-A1
优先权日:2001-04-05
标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof
发明人:READER JOHN C
权利人:MILLENNIUM PHARM INC
摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.

专利号:US-6664282-B2
优先权日:1999-09-17
标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds
发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A
权利人:TORREY PINES INST
摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.

专利号:US-5856107-A
优先权日:1997-02-04
标 题 :Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein
发明人:OSTRESH JOHN M; HOUGHTEN RICHARD A
权利人:TREGA BIOSCIENCES INC
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-2008214565-A1
优先权日:2003-04-07
标 题:Oxazolidinone Derivatives as Antimicrobials
发明人:MEHTA ANITA; RUDRA SONALI; RAO AJJARAPU VENKATA SUBRAHMANYA RAJO; YADAV AJAY SINGH; RATTAN ASHOK
权利人:MEHTA ANITA; RUDRA SONALI; RAO AJJARAPU VENKATA SUBRAHMANYA RAJO; YADAV AJAY SINGH; RATTAN ASHOK
摘要:The present invention relates to certain substituted phenyl oxazolidinones of formula I and H and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

专利号:US-2015038591-A1
优先权日:2002-05-31
标 题:Compounds, compositions and methods for the treatment of tauopathies
发明人:SNOW ALAN D; CAM JUDY A; CASTILLO GERARDO; HU QUBAI; LAKE THOMAS
权利人:PROTEOTECH INC
摘要:Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of tauopathies, such as Alzheimer's disease and Parkinson's disease, and the manufacture of medicaments for such treatment.
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合成参考文献


参考文献:10.1016/0031-9422(93)85543-z
摘要:Parsons IC, Gray AI, Hartley TG, Waterman PG. Brombyins from the stem bark of Brombya platynema. Phytochemistry. 1993 May;33(2):479–82. doi: 10.1016/0031-9422(93)85543-z.
参考文献:10.1007/s10295-006-0177-1
摘要:Ghosh S, Sachan A, Sen SK, Mitra A. Microbial transformation of ferulic acid to vanillic acid by Streptomyces sannanensis MTCC 6637. Journal of Industrial Microbiology & Biotechnology. 2006 Oct 17;34(2):131–8. doi: 10.1007/s10295-006-0177-1.
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