CAS: 886762-39-6; 3,4-Dichloro-2-Fluoroaniline

该化合物是一种卤化活性衍生物,含有分子式C6H4Cl2FN,该化合物是有机合成的多用途中间体,特别是在生产农用化学品,药品和特殊化学品方面,其独特的替代模式--在芳香环上有两个氯原子和一个氟原子--在交叉相交和核生殖替代反应中增强反应的回动性和选择性.卤素的电子提取效应提高了其在构建复杂的环环状框架方面的效用.在标准条件下,由于高度纯度和稳定性,3,4-二氯-2-氟尼线是研究人员和工业应用的可靠建筑块,需要精确地使基于厌油结构的功能化.

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CAS号908355-87-3 6,7-dichloro-3H...

合成工艺路线路线简述

    📜三氯苯置于ammonium Hydroxide,Tetrafluoroboric Acid,硫酸,硝酸,铁粉,溶剂黄146,Sodium Nitrite体系中,用 邻二甲苯,水,1,2-二氯乙烷,氯苯,丙酮 作为反应溶剂,135.0 °C,1.0 Mpa 条件下,反应 8.0H,反应生成 3,4-二氯-2-氟苯胺
    参考文献:一种3,4-二氯-2-氟苯胺的制备方法
    标题:一种3,4-二氯-2-氟苯胺的制备方法
    摘要:本发明公开了一种3,4‑二氯‑2‑氟苯胺的制备方法,其方法步骤为:(1)以1,2,3‑三氯苯为原料,经硝化反应后得到2,3,4‑三氯硝基苯;(2)所述2,3,4‑三氯硝基苯经氨解反应,得到2,3‑二氯‑6‑硝基苯胺;(3)所述2,3‑二氯‑6‑硝基苯胺在有机溶剂中与含氟无机酸和亚硝酸钠发生重氮化反应反应生成重氮盐,再加热分解得到2‑氟‑3,4‑二氯硝基苯;(4)所述2‑氟‑3,4‑二氯硝基苯经还原得到3,4‑二氯‑2‑氟苯胺.本方法以1,2,3‑三氯苯为原料,通过硝化,氨解,重氮化,分解,还原等工艺,得到3,4‑二氯‑2‑氟苯胺;本方法提供了一条3,4‑二氯‑2‑氟苯胺的合成线路,具有工艺简单,过程易控,产品收率高,纯度高以及生产成本低等特点.

    海关参考信息

    专利信息


    专利号:US-2022064145-A1
    优先权日:2020-08-28
    标 题 :Synthesis of poziotinib derivative
    发明人:BANG KEUK CHAN; MOON YOUNG HO; CHANG YOUNG KIL
    权利人:HANMI SCIENCE CO LTD
    摘要:A method for the synthesis of a compound of Formula II is provided. Also disclosed is the salt form of the compound. The method includes the introduction of a piperidinyl moiety in a polar aprotic solvent system, followed by the removal of the protecting group and the acrylation step.

    专利号:US-2021221792-A1
    优先权日:2020-01-16
    标题:Convergent synthesis of poziotinib derivative
    发明人:CHAN BANG KEUK; HYUK JUNG JAE; HO MOON YOUNG
    权利人:HANMI PHARM IND CO LTD
    摘要:A method of for the synthesis of a compound of Formula I is disclosed herein. The method includes reacting a compound of formula (II) with a compound of formula (III) in an inert polar aprotic solvent system in the presence of a base.

    专利号:WO-2022043923-A1
    优先权日:2020-08-28
    标题 :Synthesis of poziotinib derivative

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1126/science.abo7201
    摘要:Boby ML, Fearon D, Ferla M, Filep M, Koekemoer L, Robinson MC; COVID Moonshot Consortium‡, Chodera JD, Lee AA, London N, von Delft A, von Delft F, Achdout H, Aimon A, Alonzi DS, Arbon R, Aschenbrenner JC, Balcomb BH, Bar-David E, Barr H, Ben-Shmuel A, Bennett J, Bilenko VA, Borden B, Boulet P, Bowman GR, Brewitz L, Brun J, Bvnbs S, Calmiano M, Carbery A, Carney DW, Cattermole E, Chang E, Chernyshenko E, Clyde A, Coffland JE, Cohen G, Cole JC, Contini A, Cox L, Croll TI, Cvitkovic M, De Jonghe S, Dias A, Donckers K, Dotson DL, Douangamath A, Duberstein S, Dudgeon T, Dunnett LE, Eastman P, Erez N, Eyermann CJ, Fairhead M, Fate G, Fedorov O, Fernandes RS, Ferrins L, Foster R, Foster H, Fraisse L, Gabizon R, García-Sastre A, Gawriljuk VO, Gehrtz P, Gileadi C, Giroud C, Glass WG, Glen RC, Glinert I, Godoy AS, Gorichko M, Gorrie-Stone T, Griffen EJ, Haneef A, Hassell Hart S, Heer J, Henry M, Hill M, Horrell S, Huang QYJ, Huliak VD, Hurley MFD, Israely T, Jajack A, Jansen J, Jnoff E, Jochmans D, John T, Kaminow B, Kang L, Kantsadi AL, Kenny PW, Kiappes JL, Kinakh SO, Kovar B, Krojer T, La VNT, Laghnimi-Hahn S, Lefker BA, Levy H, Lithgo RM, Logvinenko IG, Lukacik P, Macdonald HB, MacLean EM, Makower LL, Malla TR, Marples PG, Matviiuk T, McCorkindale W, McGovern BL, Melamed S, Melnykov KP, Michurin O, Miesen P, Mikolajek H, Milne BF, Minh D, Morris A, Morris GM, Morwitzer MJ, Moustakas D, Mowbray CE, Nakamura AM, Neto JB, Neyts J, Nguyen L, Noske GD, Oleinikovas V, Oliva G, Overheul GJ, Owen CD, Pai R, Pan J, Paran N, Payne AM, Perry B, Pingle M, Pinjari J, Politi B, Powell A, Pšenák V, Pulido I, Puni R, Rangel VL, Reddi RN, Rees P, Reid SP, Reid L, Resnick E, Ripka EG, Robinson RP, Rodriguez-Guerra J, Rosales R, Rufa DA, Saar K, Saikatendu KS, Salah E, Schaller D, Scheen J, Schiffer CA, Schofield CJ, Shafeev M, Shaikh A, Shaqra AM, Shi J, Shurrush K, Singh S, Sittner A, Sjö P, Skyner R, Smalley A, Smeets B, Smilova MD, Solmesky LJ, Spencer J, Strain-Damerell C, Swamy V, Tamir H, Taylor JC, Tennant RE, Thompson W, Thompson A, Tomásio S, Tomlinson CWE, Tsurupa IS, Tumber A, Vakonakis I, van Rij RP, Vangeel L, Varghese FS, Vaschetto M, Vitner EB, Voelz V, Volkamer A, Walsh MA, Ward W, Weatherall C, Weiss S, White KM, Wild CF, Witt KD, Wittmann M, Wright N, Yahalom-Ronen Y, Yilmaz NK, Zaidmann D, Zhang I, Zidane H, Zitzmann N, Zvornicanin SN. Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors. Science. 2023 Nov 10;382(6671):eabo7201.
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