CAS: 194798-83-9; 2-(2,4-Difluorophenyl)-1,3-Di(1H-1,2,4-Triazol-1-yl)Propan-2-Yl Dihydrogen Phosphate

该化合物是一种属于三甲醇类的抗排剂,主要用于治疗真菌感染.它是一种青氟甲醇,意是将它转化成体内的活性形态.该物质展示出广泛的抗氟甲醇活动,特别是针对Candida物种和新红外线动物的抗氟甲醇活动.Fosfluconazole的特征是口服生物利用率高和有利于细胞生长的药用植物特征,允许进行有效的系统治疗.它通常以磷酸盐形式施用,这能增加其溶解性和吸收能力.行动机制包括抑制真菌细胞细胞细胞P450酶,特别是14-demotha酶,这对雌雄性腺素合成至关重要,是真菌细胞脑膜的重要成分.这种破坏导致脑膜渗透性增加,最终导致细胞死亡.Fosfluconolol普遍得到很好的解析,其副作用类似于氟化磷的副作用,可以增强溶液的溶性能和吸收性.该物质包括可能受损的气态性肝素,特别是高压的气压.

结构式图片

上下游产品

福司氟康唑杂质e Dibenzyl 2-(2,4-Difluorophenyl)-1,3-Bis(1H-1,2,4-Triazole-1-yl)-2-Propyl Phosphate 194602-25-0
氟康唑 Fluconazole 86386-73-4

合成工艺路线路线简述

    📜2-(2,4-Difluorophenyl)-1,3-Bis(1H-1,2,4-Triazol-1-yl)Propan-2-Yl Phosphate Diammonium Salt置于甲酸体系中,化学反应 1.0H,以98.8%的收率获得磷康唑
    参考文献:一种福司氟康唑的制备方法
    标题:一种福司氟康唑的制备方法
    摘要:本发明提供了一种福司氟康唑的制备方法,包括以下步骤:制备二氯磷酸氟康唑酯:在氮气保护下,控制温度‑10~0°C,向三乙胺的二氯甲烷溶液中缓慢滴加三氯氧磷,滴完后,维持温度‑10~0oc搅拌1小时,缓慢滴加氟康唑的二氯甲烷溶液,Tlc监测反应完成;维持温度‑10~0°C,加入水搅拌30分钟,添加无机碱至水相ph至少为8,静置分层,分出上层水相,有机相内含二氯磷酸氟康唑酯,通过氟康唑‑二氯磷酸氟康唑酯‑氟康唑二苄基磷酸酯‑福司氟康唑铵盐‑福司氟康唑流程制备福司氟康唑,提高收率,可控得制备各中间体,原料可回收重复使用,减少原料浪费与有机废物污染.

    海关参考信息

    专利信息


    专利号:US-11944609-B1
    优先权日:2023-06-16
    标题:Antifungal ionic liquid and Amphotericin B combination
    发明人:RATHER SAMI-ULLAH; WANI MOHMMAD YOUNUS; BAMUFLEH HISHAM S; ALHUMADE HESHAM; SAEED USMAN; TAIMOOR AQEEL AHMAD; ALALAYAH WALID M; RATHER IRFAN AHMAD
    权利人:KING ABDULAZIZ UNIVERISTY; UNIV KING ABDULAZIZ
    摘要:Provided herein are ionic liquids that can be used as antifungal agents alone or in combination with Amphotericin B. Also disclosed are methods of synthesis of the ionic liquids and inhibiting fungal growth and methods of treating fungal infections using the disclosed compounds. The disclosure provides antifungal agents that potentiate the antifungal activity of Amphotericin B, a commonly used antifungal drug that could be used alone or in combination. This combination will help control and combat the infections caused by drug resistant Candida. auris in immunocompromised patients.

    专利号:US-2012172336-A2
    优先权日:2009-03-19
    标 题:Fosfluconazole Derivatives, Synthesis, and Use in Long Acting Formulations
    发明人:GONNISSEN YVES; VOORSPOELS JODY
    权利人:GONNISSEN YVES; VOORSPOELS JODY; SEPS PHARMA N V
    摘要:The invention relates to a compound of formula (1) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R 1 to R 2 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.

    专利号:WO-2020123881-A1
    优先权日:2018-12-12
    标题:Boron containing compounds and their uses
    发明人:LIU CHUN YU; ZHOU YASHEEN; YANG STEPHEN; LIU CBUNLIANG; ZHANG YONG-KANG
    权利人:BORAGEN INC
    摘要:The present disclosure relates to boron-containing compounds, novel combiantions, and novel uses. The disclosure provides novel benzoxaborole compounds, pharmaceutical compositions, and associated methods of use. In particular, modeling suggests the benzoxaborole compounds disclosed herein are useful for inhibiting protein prenylation or ergosterol synthesis in a pathogenic microorganism. The benzoxaborole compounds according to the disclosure are further useful for the treatment of infectious microorganisms including pathogenic fungi and protozoan parasites, such as those that cause malaria.

    专利号:RU-2176244-C2
    优先权日:1996-02-02
    标题:Derivatives of triazole, methods of their synthesis, pharmaceutical composition, method of treatment and prophylaxis of fungal infections, intermediate compound

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Hagiya H, Kajioka H. Successful treatment of recurrent candidemia due to candidal thrombophlebitis associated with a central venous catheter using a combination of fosfluconazole and micafungin. Intern Med. 2013;52(18):2139-43. doi: 10.1111/j.1365-2710.2011.01297.x. Epub 2011 Aug 24. Japanese. doi: 10.1155/2009/274768. Epub 2009 Apr 23.
    5: Aoyama T, Ogata K, Shimizu M, Hatta S, Masuhara K, Shima Y, Kimura K, Matsumoto Y. Pharmacokinetics of fluconazole and fosfluconazole after intraperitoneal administration to peritoneal dialysis rats. Drug Metab Pharmacokinet. 2005 Dec;20(6):485-90.
    7: Kawakami Y, Nagino K, Shinkai K, Sobue S, Abe M, Ishiko J. [Nonclinical studies and clinical studies on fosfluconazole, a triazole antifungal agent (Prodif)]. Nihon Yakurigaku Zasshi. 2004 Jul;124(1):41-51. Review. Japanese.

    合成参考文献


    参考文献:10.1111/j.1365-2125.2004.02073.x
    摘要:Sobue S, Tan K, Layton G, Leclerc V, Weil A. The effects of renal impairment on the pharmacokinetics and safety of fosfluconazole and fluconazole following a single intravenous bolus injection of fosfluconazole. Brit J Clinical Pharma. 2004 Apr 21;57(6):773–84. doi: 10.1111/j.1365-2125.2004.02073.x.
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