CAS: 36404-90-7; 2-Fluoronicotinaldehyde

该化合物是一个多功能的氟化环环状构件,广泛用于制药和农用化学合成,其主要结构特征包括三点方位的活性aldhyde小组和双点方位的氟化物替代体,这对电子特性有重大影响,并提高药物候选体的代谢稳定性.该化合物是合成各种生物活性分子的宝贵前体,特别是在发展动脉抑制剂和其他治疗剂方面.其高纯度和定义明确的再活动使得它特别有助于核分裂性附加反应,凝聚反应和过渡性金属催化交叉组合过程.氟和甲醚的功能的存在可以进行多种结构修改,从而能够高效地构建复杂的分子结构.

结构式图片

相似化合物

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CAS号2591-86-8 1-甲酰哌啶 | CAS号372-48-5 2-氟吡啶 | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号131747-55-2 2-氟-3-(羟甲基)吡啶 | CAS号119899-26-2 2-氟烟酰氯 | CAS号1603-40-3 2-氨基-3-甲基吡啶 | CAS号2369-18-8 2-氟-3-甲基吡啶 | CAS号393-55-5 2-氟烟酸 | CAS号766-11-0 5-溴-2-氟吡啶 | CAS号109-94-4 甲酸乙酯 | CAS号68618-36-0 3-溴-1H-吡唑并[3,4B]吡啶 | CAS号1319591-26-8 3-(4,4,5,5-四甲基-... | CAS号131747-55-2 2-氟-3-(羟甲基)吡啶 | CAS号271-73-8 1H-吡唑并[3,4-b]吡啶

合成工艺路线路线简述

    2-氨基-3-甲基吡啶置于potassium Permanganate,Lithium Aluminium Tetrahydride,Tetrafluoroboric Acid,磷酸,氯甲酸乙酯,二甲基亚砜,三乙胺,N,N'-二环己基碳二亚胺,Sodium Nitrite体系中,用 水 用作溶剂,化学反应 3.0H,反应生成2-氟烟醛
    参考文献:新型1,4-二氢吡啶类钙拮抗剂.I.4-(取代的吡啶基)-1,4-二氢吡啶衍生物的合成和降血压活性.
    标题:新型1,4-二氢吡啶类钙拮抗剂.I.4-(取代的吡啶基)-1,4-二氢吡啶衍生物的合成和降血压活性.
    摘要:合成了一系列4-(取代的吡啶基)-1,4-二氢吡啶衍生物,并研究了它们的降压作用.几种化合物,2-(n-苄基-N-甲基氨基)乙基甲基1,4-二氢-2,6-二甲基-4-(3-硝基-2-吡啶基)-3,5-吡啶二甲酸(2B),4-(4-硝基-2-吡啶基)类似物(2G),4-(3-三氟甲基-2-吡啶基)类似物(2C),4-(2-三氟甲基-3-吡啶基)类似物(3E),4-发现(4-氰基-2-吡啶基)类似物(2E),4-(2-氰基-3-吡啶基)类似物(3D)和4-(6-溴-2-吡啶基)类似物(2I)具有与尼卡地平类似的降压活动;特别是2C和3E的持续时间约为尼卡地平的两倍,而2E具有在所有合成衍生物中最有效的降压活性.
    Doi:10.1248/cpb.38.2446

    海关参考信息

    专利信息


    专利号:US-2004053355-A1
    优先权日:2000-05-26
    标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors
    发明人:WAINER IRVING; MARKOGLOU NEKTARIA
    摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.

    专利号:US-9574189-B2
    优先权日:2005-12-01
    标题:Enzymatic encoding methods for efficient synthesis of large libraries
    发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
    权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
    摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).

    专利号:US-11225655-B2
    优先权日:2010-04-16
    标题:Bi-functional complexes and methods for making and using such complexes
    发明人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK
    权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS
    摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

    专利号:US-11702652-B2
    优先权日:2005-12-01
    标题:Enzymatic encoding methods for efficient synthesis of large libraries

    专利号:US-2009264300-A1
    优先权日:2005-12-01
    标题 :Enzymatic encoding methods for efficient synthesis of large libraries

    专利号:US-2020216836-A1
    优先权日:2005-12-01
    标题 :Enzymatic encoding methods for efficient synthesis of large libraries
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    合成参考文献


    参考文献:10.1055/s-0030-1258198
    摘要:Bräse S, Allendörfer N, Es-Sayed M, Nieger M. Novel Aromatic Fluoroolefins via Fluoro-Julia-Kocienski Olefination. Synthesis. 2010 Aug 05;2010(20):3439–48. doi: 10.1055/s-0030-1258198.
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