CAS: 239807-03-5; Voriconazole Impurity 8

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    (2R,3S/2S,3R)-3-(6-氯-5-氟嘧啶-4-基)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇盐酸盐 3-(6-Chloro-5-Fluoropyrimidin-4-yl)-2-(2,4-Difluorophenyl)-1-(1H-1,2,4-Triazol-1-yl)-2-Butanol 188416-35-5

    合成工艺路线路线简述

      📜(2R,3S/2S,3R)-3-(6-氯-5-氟嘧啶-4-基)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇盐酸盐置于palladium 10% On Activated Carbon 氢气,Sodium Acetate体系中,用 水,乙酸乙酯 用作溶剂,25.0~30.0 °C,490.34 Kpa 条件下,反应生成伏立康唑杂质8
      参考文献: Process For The Preparation Of Voriconazole[fr] Procédé De Préparation De Voriconazole
      标题: Process For The Preparation Of Voriconazole[fr] Procédé De Préparation De Voriconazole
      摘要:本发明提供了一种在单个反应容器中制备顺式伏立康唑的方法.本发明还提供了一种使用顺式伏立康唑制备伏立康唑的方法以及与之相关的制备过程.

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      主要参考文献


      1: Maertens JA, Raad II, Marr KA, Patterson TF, Kontoyiannis DP, Cornely OA, Bow EJ, Rahav G, Neofytos D, Aoun M, Baddley JW, Giladi M, Heinz WJ, Herbrecht R, Hope W, Karthaus M, Lee DG, Lortholary O, Morrison VA, Oren I, Selleslag D, Shoham S, Thompson GR 3rd, Lee M, Maher RM, Schmitt-Hoffmann AH, Zeiher B, Ullmann AJ. Isavuconazole versus voriconazole for primary treatment of invasive mould disease caused by Aspergillus and other filamentous fungi (SECURE): a phase 3, randomised-controlled, non-inferiority trial. Lancet. 2016 Feb 20;387(10020):760-9. doi: 10.1016/S0140-6736(15)01159-9. Epub 2015 Dec 10. 212(1):157-165. doi: 10.2214/AJR.18.19991. Epub 2018 Nov 7. 36(5):786-95. doi: 10.1055/s-0035-1562903. Epub 2015 Sep 23. 78(11):2630-2636. doi: 10.1093/jac/dkad293. 181(18):V12180870. Danish. 15(5):493-502. doi: 10.1080/14787210.2017.1305886. Epub 2017 Mar 24. 88(12):5166-5182. doi: 10.1111/bcp.15495. Epub 2022 Aug 25. 28(3):e671. doi: 10.1097/RHU.0000000000001850. 50(7):489-494. doi: 10.1080/23744235.2017.1418531. Epub 2017 Dec 20. 51(3):247-265. doi: 10.1080/03602532.2019.1632888. Epub 2019 Aug 16. 27(2):151-160. doi: 10.1016/j.jiac.2020.11.014. Epub 2020 Dec 26. 61(4):106750. doi: 10.1016/j.ijantimicag.2023.106750. Epub 2023 Feb 8. 66(9):e0017722. doi: 10.1128/aac.00177-22. Epub 2022 Aug 15.
      14: Zhong X, Tong X, Ju Y, Du X, Li Y. Interpersonal Factors in the Pharmacokinetics and Pharmacodynamics of Voriconazole: Are CYP2C19 Genotypes Enough for Us to Make a Clinical Decision? Curr Drug Metab. 2018;19(14):1152-1158. doi: 10.2174/1389200219666171227200547.
      15: Kadam RS, Van Den Anker JN. Pediatric Clinical Pharmacology of Voriconazole: Role of Pharmacokinetic/Pharmacodynamic Modeling in Pharmacotherapy. Clin Pharmacokinet. 2016 Sep;55(9):1031-43. doi: 10.1007/s40262-016-0379-2.
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