CAS: 909036-46-0; 2-Chloro-3-Iodopyridin-4-Amine

该化合物是一种卤化的衍生物,在制药和农用化学合成方面有很大的用途,其2个和3个位置的不同替代模式-氯和碘组,以及4位置的氨基氨基生物组-使它成为交叉反应的多用途中间体,如Suzuki或Buchwald-Hartwig 喷射;用电排出卤素增强回活动,而氨基亚基亚基组则为进一步的功能化提供处理器;这一化合物对于生物活性分子的环环形手架的开发特别有价值;在标准储存条件下的高纯度和稳定性确保合成应用的一贯性能.

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相似化合物

1235873-11-6 1171919-00-8 800402-12-4

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CAS号14432-12-3 4-氨基-2-氯吡啶 | CAS号234108-74-8 (2-氯-3-碘-4-吡啶)氨... | CAS号854018-87-4 4-氯-2-甲基-1H-吡咯并...

合成工艺路线路线简述

  • 合成目标产物 2-Chloro-3-Iodopyridin-4-Amine 主要起始原料 4-Amino-2-Chloropyridine
  • 14432-12-3 = 909036-46-0
    反应条件:1.1 Reagents: Sodium Acetate,Iodine Chloride Solvents: Acetic Acid; 16 H,70 °C1.2 Reagents: Sodium Bicarbonate Solvents: Ethyl Acetate,Water
    标题:Synthesis And Trypanocidal Activity Of A Library Of 4-Substituted 2-(1H-Pyrrolo[3,2-C]Pyridin-2-Yl)Propan-2-Ols
    作者:Balfour,Michael N.; Franco,Caio H.; Moraes,Carolina B.; Freitas-Junior,Lucio H.; Stefani,Helio A.
    参考文献:European Journal Of Medicinal Chemistry 日期:2017 卷标:128 页码:202-212]

    14432-12-3 = 909036-46-0
    反应条件:1.1 Reagents: N-Iodosuccinimide Solvents: Dimethylformamide; 18 H,55 °C
    标题:Structure-Activity Relationships And Structure-Kinetic Relationships Of Pyrrolopiperidinone Acetic Acids As Crth2 Antagonists
    作者:Andres,Miriam; Buil,Maria Antonia; Calbet,Marta; Casado,Oscar; Castro,Jordi; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2014 卷标:24(21) 页码:5111-5117]

    14432-12-3 = 909036-46-0
    反应条件:1.1 Reagents: Acetic Acid,Sodium Acetate,Iodine Chloride; Rt; 16 H,70 °C
    标题:Identification Of 2,4-Disubstituted Imidazopyridines As Hemozoin Formation Inhibitors With Fast-Killing Kinetics And In Vivo Efficacy In The Plasmodium Falciparum Nsg Mouse Model
    作者:Horatscheck,Andre; Andrijevic,Ana; Nchinda,Aloysius T.; Le Manach,Claire; Paquet,Tanya; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2020 卷标:63(21) 页码:13013-13030]

    14432-12-3 = 909036-46-0 + 800402-12-4
    反应条件:1.1 Reagents: Potassium Acetate,Iodine Chloride Solvents: Acetic Acid; 60 - 70 °C
    标题:Potent 4-Amino-5-Azaindole Factor Viia Inhibitors
    作者:Hu,Huiyong; Kolesnikov,Aleksandr; Riggs,Jennifer R.; Wesson,Kieron E.; Stephens,Robin; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2006 卷标:16(17) 页码:4567-4570]

    14432-12-3 = 909036-46-0 + 1171919-00-8 + 800402-12-4
    反应条件:1.1 Reagents: Potassium Acetate,Iodine Chloride Solvents: Acetic Acid; 4 H,Rt -> 70 °C1.2 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized
    标题:Synthesis,Crystal Structure,Molecular Docking And Antimicrobial Evaluation Of New Pyrrolo[3,2-C]Pyridine Derivatives
    作者:Jose,Gilish; Suresha Kumara,T. H.; Nagendrappa,Gopalpur; Sowmya,H. B. V.; Jasinski,Jerry P.; Et Al
    参考文献:Journal Of Molecular Structure 日期:2015 卷标:1081 页码:85-95]

    14432-12-3 = 909036-46-0 + 1171919-00-8 + 800402-12-4
    反应条件:1.1 Reagents: Potassium Acetate,Iodine Chloride Solvents: Water; 4 D,Ph 5.5,75 °C1.2 Reagents: Sodium Carbonate Solvents: Water; Ph 7 - 8,Rt1.3 Reagents: Sodium Thiosulfate Solvents: Water; Rt
    标题:Palladium-Catalyzed Synthesis Of 2,3-Disubstituted 5-Azaindoles Via Heteroannulation Reaction And Of 2-Substituted 5-Azaindoles Through Domino Sila-Sonogashira/5-Endo Cyclization
    作者:Livecchi,Marion; Calvet,Geraldine; Schmidt,Frederic
    参考文献:Journal Of Organic Chemistry 日期:2012 卷标:77(11) 页码:5006-5016]

    14432-12-3 = 909036-46-0 + 1171919-00-8 + 800402-12-4
    反应条件:1.1 Reagents: Potassium Acetate,Iodine Chloride Solvents: Acetic Acid; 4 H,Rt -> 70 °C1.2 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized
    标题:New Polyfunctional Imidazo[4,5-C]Pyridine Motifs: Synthesis,Crystal Studies,Docking Studies And Antimicrobial Evaluation
    作者:Jose,Gilish; Suresha Kumara,T. H.; Nagendrappa,Gopalpur; Sowmya,H. B. V.; Jasinski,Jerry P.; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2014 卷标:77 页码:288-297]

    14432-12-3 = 909036-46-0 + 1171919-00-8 + 800402-12-4
    反应条件:1.1 Reagents: Potassium Acetate,Iodine Chloride Solvents: Acetic Acid; 4 H,70 °C
    标题:Synthesis,Molecular Docking,Antimycobacterial And Antimicrobial Evaluation Of New Pyrrolo[3,2-C]Pyridine Mannich Bases
    作者:Jose,Gilish; Suresha Kumara,Tholappanavara H.; Sowmya,Haliwana B. V.; Sriram,Dharmarajan; Guru Row,Tayur N.; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2017 卷标:131 页码:275-288
📜2-氯-4-氨基吡啶置于sodium Acetate Trihydrate,一氯化碘,溶剂黄146体系中,化学反应 16.0H,以45%的收率获得产物2-氯-3-碘-4-吡啶胺
参考文献:4-取代的2-(1 H-吡咯并[3,2-C]吡啶-2-基)丙烷-2-醇的文库的合成和锥虫活性
标题:4-取代的2-(1 H-吡咯并[3,2-C]吡啶-2-基)丙烷-2-醇的文库的合成和锥虫活性
摘要:16 4-取代的2-(1的文库ħ吡咯并[3,2-C ^]吡啶-2-基)丙-2-醇17-32已被用于合成在抗生物测试克氏锥虫,原生动物寄生虫导致恰加斯病.四取代的2-(1 ħ吡咯并[3,2-C ^]吡啶-2-基)丙-2-醇17-32进行生物测试,以抗胞内评估其疗效克氏锥虫(y株)以苯甲硝唑为参照化合物感染u2Os人细胞的变形虫.一式两份进行该测定(两个独立实验),并进行高含量分析(hca)以测定锥虫活性.所测试的化合物的三呈现相对高的杀锥虫活性(19,22和29)中,观测到严重然而宿主细胞毒性伴随.将需要对高活性化合物进行化学优化并合成更多化合物以用于针对克鲁氏锥虫的生物学测试,以提高选择性,从而可以建立结构-活性关系,以提供对化学和生物学方面的更深入的分析.
DOI:10.1016/j.Ejmech.2017.01.040

海关参考信息

专利信息


专利号:US-9708336-B2
优先权日:2014-01-22
标题 :Metallo-beta-lactamase inhibitors
发明人：MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

专利号:CA-3236558-A1
优先权日:2021-10-29
标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound

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主要参考文献

参考标题:Metallo-Beta-Lactamase Inhibitors
摘要:The Present Invention Relates To Compounds Of Formula (I) That Are Metallo-β-Lactamase Inhibitors, The Synthesis Of Such Compounds, And The Use Of Such Compounds For Use With β-Lactam Antibiotics For Overcoming Resistance.

合成参考文献

参考DOI号:10.1016/j.ejmech.2014.03.019
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