CAS: 327-92-4; 1,5-Difluoro-2,4-Dinitrobenzene

该化合物是一种氟芳烃化合物,其特征为1和5位置的两个硝基化合物和氟替代物.该结构具有高度的回活动性,使其成为有机合成中有价值的中间体,特别是对于核生殖性替代反应而言尤其如此.电排硝基子组增强了芳香环的电益性,促进了选择性功能化.其氟基原子进一步促进了其在制造复合分子(如制药和农用化学物质)方面的用途.该化合物在标准条件下的稳定性确保了处理和储存的便利性.其精确的回活动状态允许有控制的修改,使它成为细微化学应用的首选.

结构式图片

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CAS号372-18-9 1,3-二氟苯 | CAS号3698-83-7 1,3-二氯-4,6-二硝基苯 | CAS号446-35-5 2,4-二氟硝基苯 | CAS号367-81-7 2,4-二硝基-5-氟苯胺 | CAS号4987-96-6 4,6-二硝基-1,3-苯二胺 | CAS号142744-18-1 3-N-[2-[[5-[(di... | CAS号142744-23-8 1-N-[2-[[5-[(di... | CAS号142744-25-0 N-[2-[[5-[(dime... | CAS号142744-17-0 1,3-Benzenediam... | CAS号142744-26-1 1-N-[2-[[5-[(di... | CAS号142744-21-6 1-N-[2-(dimethy... | CAS号25917-90-2 2-甲氧基-5-硝基苯-1,4-二胺 | CAS号616-74-0 4,6-二硝基间苯二酚

合成工艺路线路线简述

  • 合成目标产物 1,5-Difluoro-2,4-Dinitrobenzene 主要起始原料 2,4-Difluoronitrobenzene
  • (文献来源)合成步骤主要原料 2,4-Difluoronitrobenzene
1,3-二氟苯置于硫酸,硝酸体系中,用93%的收率获得1,5-二氟-2,4-二硝基苯
参考文献:5-氨基-2,4,6-三硝基-1,3-二羟基苯的合成与爆轰性能.
标题:5-氨基-2,4,6-三硝基-1,3-二羟基苯的合成与爆轰性能.
摘要:通过大环化合物4的开环反应,借助vns(氢的亲核取代)反应条件,合成了5-氨基-4,6-二硝基-1,3-二羟基苯(6) .研究了大环化合物4的开环 机理.在kno 3和浓硫酸中将6硝化后,得到5-氨基-2,4,6,三硝基-1,3-二羟基苯(8).6或8的热稳定性,灵敏度和其他爆震性能分别与市售的1,3,5-三氨基-2,4,6-三硝基苯(tatb)或1,3,5-三硝基三氮杂环己烷(rdx)进行了比较.所有目标化合物均通过单晶x射线衍射,NMR光谱,元素分析和差示扫描量热法进行了表征.敏感性通过bam方法(落锤和摩擦测试)确定.使用gaussian 03和explo5 V6.01程序分别计算了性能参数,包括地层热和爆轰性能.值得指出的是,化合物 8在298 K下的实测密度为2.078 G Cm-3.此外,化合物 8比rdx更不敏感(化合物 8:Is= 11J;Rdx:Is = 7 J;Is是撞击灵敏度).
Doi:10.1002/open.201600132

专利信息


专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人:COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-10254287-B2
优先权日:2015-07-21
标题 :Protein fluorescent nanoparticles and methods of synthesis thereof
发明人:KUMAR CHALLA VIJAYA; STROMER BOBBI SHANYELLE
权利人:UNIV CONNECTICUT
摘要:Disclosed herein are stable and versatile protein nanoparticles having a range of tunable fluorescent properties. Such nanoparticles may find utility in biological imaging. Methods of synthesis of such nanoparticles are also disclosed.

专利号:US-2008267981-A1
优先权日:2004-06-30
标题:Compositions and Methods for Delivery of Antitumor Agents
发明人:JANDA KIM D; WIRSCHING PETER; BOGER DALE L
权利人:SCRIPPS RESEARCH INST
摘要:Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.
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合成参考文献


参考文献:10.1021/ol025725h
摘要:Shivanyuk A, Far AR, Rebek J. Rigid tetranitroresorcinarenes. Org Lett. 2002 May 02;4(9):1555–8. doi: 10.1021/ol025725h.
参考文献:10.1016/j.chroma.2008.02.084
摘要:Bhushan R, Kumar V. Synthesis of chiral hydrazine reagents and their application for liquid chromatographic separation of carbonyl compounds via diastereomer formation. J Chromatogr A. 2008 May 09;1190(1-2):86–94. doi: 10.1016/j.chroma.2008.02.084.
参考文献:10.1111/j.1432-1033.1985.tb09216.x
摘要:Trexler M, Bányai L, Patthy L, Pluck ND, Williams RJ. Chemical modification and nuclear magnetic resonance studies on human plasminogen kringle 4. Assignment of tyrosine and histidine resonances to specific residues in the sequence. Eur J Biochem. 1985 Oct 15;152(2):439–46. doi: 10.1111/j.1432-1033.1985.tb09216.x.
参考文献:10.1007/s002329900585
摘要:Flötenmeyer M, Momayezi M, Plattner H. Hydrophobic and Hydrophilic Radio-Iodination, Crosslinking, and Differential Extraction of Cell Surface Proteins in Paramecium tetraurelia Cells. The Journal of Membrane Biology. 1999 Nov;172(1):77–88. doi: 10.1007/s002329900585.
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