CAS: 64872-76-0; 1-(4-(4-Chlorophenyl)-2-((2,6-Dichlorophenyl)Thio)Butyl)-1H-Imidazole

该化合物是一种具有独特结构结构配置的氯化imidazole衍生物,具有芳香和含硫功能组别,该化合物因其反应场所而具有作为制药和农用化学合成中间体的潜力,允许进一步发挥功能;多种氯代基体的存在增强了其稳定性,并可能促进生物活动,使其成为研究抗微生物或抗硫应用的候选体;其定义明确的分子结构确保合成工艺的再生性,而硫基联系在化学改造中具有多功能性;对于受控实验室使用而言,需要根据标准安全议定书处理,因为其卤化性质.

结构式图片

上下游产品

1-[2-chloro-4-(4-chlorophenyl)-n-butyl]imidazole 2,6-dichlorothiophenol 1-Chloro-4-(chloromethyl)benzene 1-chloro-4-(4-chlorophenyl)-2-butanol-1H-imidazole(2R)-1-2-(2,6-dichlorophenylthio)-4-(4-chlorophenyl)butyl-1H-imidazole -1H-imidazole(2S)-1-2-(2,6-dichlorophenylthio)-4-(4-chlorophenyl)butyl-1H-imidazole (-)-but°Conazole (+)-but°Conazole

合成工艺路线路线简述

    1-氯-4-(4-氯苯基)-2-丁醇置于氯化亚砜,Sodium Hydride,Potassium Carbonate体系中,用 N,N-二甲基甲酰胺,丙酮 作为反应溶剂,化学反应 27.5H,反应生成 布康唑
    参考文献:一种硝酸布康唑的制备方法
    标题:一种硝酸布康唑的制备方法
    摘要:本发明公开了一种硝酸布康唑的制备方法.以4‑氯苄基氯为起始原料合成1‑氯‑4‑(4‑氯苯基)‑2‑丁醇,再合成1‑(4‑(4‑氯苯基)‑2‑羟基‑丁基)咪唑,然后再合成1‑(4‑(4‑氯苯基)‑2‑氯‑丁基)咪唑,将1‑(4‑(4‑氯苯基)‑2‑氯‑丁基)咪唑,2,6‑二氯苯硫酚,碳酸钾加入到丙酮中,加热回流,反应完成后加入水和乙酸乙酯,分液,乙酸乙酯相依次用饱和碳酸钾和饱和食盐水洗涤,无水硫酸镁干燥,去除硫酸镁后,冰浴下滴加65%的硝酸,至无沉淀产生,过滤收集固体,用无水乙醇重结晶,得白色晶体,即硝酸布康唑.本发明的一种硝酸布康唑的制备方法,工艺简单,收率高,成本低,得到的产品纯度高.

    海关参考信息

    专利信息


    专利号:US-11311505-B2
    优先权日:2017-02-24
    标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

    专利号:US-10813893-B2
    优先权日:2017-02-24
    标 题:Compositions and methods for the treatment and prevention of chronic hypoxemia and dyspnea
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:The present invention has shown that not all salts of pyruvic acid enhance lung functions or enhance the synthesis of lung surfactants and that certain salts of pyruvic acid with the correct concentrations of calcium, phosphate and magnesium, are synergistic in their ability to enhance the synthesis of lung surfactants that will enhance lung alveoli functions, while decreasing coughing and lung tightness, and increasing oxygen saturation values to prevent hypoxemia. This patent demonstrates that the sodium pyruvate formula with calcium, phosphate and magnesium was superior over standard sodium pyruvate formula in saline alone in the removal of mucus, reduction of lung or sinus infections, and in reducing drug side effects and congestion. The use of this formula clearly demonstrated that it can be used to produce better efficacy in patients with hypoxemia, with lung and sinus diseases including, asthma, COPD, cystic fibrosis, interstitial lung disease, allergic rhinitis, sinusitis, Alzheimer's, disease, Parkinson's disease, brain trauma, nicotine addiction, sleep apnea, autism, migraine headaches, sleep disorders, lung and sinus infections, cancer therapy with cancer drugs, nicotine addiction, and medications that cause a decrease in lung surfactants.

    专利号:WO-2025085030-A1
    优先权日:2023-10-18
    标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring
    发明人:SARIPINAR EMIN; BURAN SUMEYYE
    权利人:ERCIYES UNIV
    摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.

    专利号:US-11628186-B2
    优先权日:2017-02-24
    标题 :Method and composition for the reduction of viral replication, duration and spread of the COVID-19 and the flu
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:A method for stimulating the synthesis of nasal nitric oxide and nasal and lung surfactants to inhibit the docking and adhesion of viruses to cellular receptors, including ACE2, to reduce viral replication, duration, spread and severity of infections, and also to inhibit lung fibrosis, increase the synthesis of serotonin to reduce coughing and mouth breathing, reduce the cytokine storm produced by LI-6 caused by viruses such as COVID-19 and flu in patients susceptible to these infections, including patients with hypoxemia, asthma, chronic obstructive pulmonary disease, cystic fibrosis, diabetics, interstitial lung disease, pulmonary fibrosis, allergic rhinitis, sinusitis, smokers, sleep apnea and lung cancer, which includes: contacting mammalian cells with a therapeutically effective amount of a composition, said composition including the following constituents: sodium pyruvate; a phosphate; a salt of calcium; and a salt of magnesium.

    专利号:WO-2025085026-A1
    优先权日:2023-10-18
    标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring
    发明人:SARIPINAR EMIN; BURAN SUMEYYE
    权利人:T C ERCIYES UNIV
    摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.

    专利号:US-2024336559-A1
    优先权日:2021-10-06
    标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
    发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA
    权利人:UNIV NEW YORK STATE RES FOUND
    摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
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    主要参考文献


    1: Jia MM, Zhou Y, He XM, Wu YL, Li HQ, Chen H, Li WY. Development of a liquid chromatography-tandem mass spectrometry method for determination of butoconazole nitrate in human plasma and its application to a pharmacokinetic study. J Huazhong Univ Sci Technolog Med Sci. 2014 Jun;34(3):431-6. doi: 10.1007/s11596-014-1296-y. Epub 2014 Jun 18.
    11: Lappin MA, Brooker DC, Francisco CA, Dorfman J. Effect of butoconazole nitrate 2% vaginal cream and miconazole nitrate 2% vaginal cream treatments in patients with vulvovaginal candidiasis. Infect Dis Obstet Gynecol. 1996;4(6):323-8.
    12: Brown D Jr, Henzl MR, LePage ME, Tsao LL, Izu AE, Walker KA, Adamson GD, Droegmuller W. Butoconazole vaginal cream in the treatment of vulvovaginal candidiasis. Comparison with miconazole nitrate and placebo. J Reprod Med. 1986 Nov;31(11):1045-8.

    合成参考文献


    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from
    摘要:Heng LZ, Chen Y, Tan TC. Treatment of recurrent vulvo-vaginal candidiasis with sustained-released butoconazole pessary. Singapore Med J. 2012 Dec;53(12):e269–71.
    摘要:Bourée P, Issoire C. [In vitro evaluation of the activity of butoconazole against Trichomonas vaginalis]. Pathol Biol (Paris). 1992 May;40(5):492–4.
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