CAS: 99592-32-2; 1-[2-[(7-Chloro-1-Benzothiophen-3-yl)Methoxy]-2-(2,4-Dichlorophenyl)Ethyl]Imidazole

该化合物是一种属于imidazole类的广频抗软体剂,主要用于治疗皮肤植物素,皮肤直线虫病和其他表面真菌感染,其行动机制包括抑制egosterol生物合成,破坏真菌细胞膜的完整性.Sertaconazole展示了针对Trichophyton,Candida和Malassazia物种的有力活动,许多菌株的抑制浓度很低.该化合物显示出有利的药用植物特性,包括强固的皮肤保留和最小的系统吸收,在减少系统接触的同时提高局部效力,其抗炎和抗酸性效应进一步有助于临床在管理症状性感染方面的效用.Sertaconazole是用于定向应用,确保患者遵守和耐受耐受性,用于热剂的热剂(奶,粉剂)中的配方.

结构式图片

欧盟法规

C&L通报

上下游产品

(7-Chlorobenzo[b]Thiophen-3-yl)Methanol
Alpha-(2,4-二氯苯基)-1H-咪唑-1-乙醇 1-(2,4-Dichlorophenyl)-2-(1H-Imidazol-1-yl)Ethan-1-Ol 24155-42-8

合成工艺路线路线简述

    (2-Chloro-6-Iodophenyl)(Prop-2-Yn-1-yl)Sulfane置于potassium Tert-Butylate,[au2(μ-Bis(Diphenylphosphino)Methane)2](Otf)2,四丁基碘化铵,Sodium Carbonate,甲基磺酰氯,三乙胺,Sodium Hydroxide体系中,用 四氢呋喃,二氯甲烷,水,甲苯,乙腈 作为反应溶剂,化学反应 20.5H,反应生成 舍他康唑
    参考文献:通过金催化剂和芳基碘化物之间的三重能量转移可见光诱导自由基碳环化/宝石二硼化
    标题:通过金催化剂和芳基碘化物之间的三重能量转移可见光诱导自由基碳环化/宝石二硼化
    摘要:Geminal二硼酸盐因其独特的结构和反应性而引起了极大的关注.然而,基于苯并呋喃,吲哚和苯并噻吩的苄基宝石二硼酸酯(生物相关化合物的构建单元)尚不清楚.提出了一种使用可见光和芳基碘化物构建有价值的构建模块的有前途的协议,包括苯并呋喃,吲哚和苯并噻吩基苄基二硼酸酯,通过具有高官能团耐受性的炔烃的自由基碳环化/宝石二硼化.这些宝石二硼酸盐的效用已通过 10 克规模的转换,多功能转化,包括合成批准的药物支架和两种批准的药物,甚至聚合物合成得到证明.
    DOI:10.1021/jacs.0C03197

    海关参考信息

    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    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: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.

    专利号:US-9382288-B2
    优先权日:2010-10-06
    标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
    发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
    权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
    摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

    专利号:US-10443047-B2
    优先权日:2014-05-01
    标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
    发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
    权利人:NOVOGY INC
    摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
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    主要参考文献

    1. Croxtall JD, Plosker GL. Sertaconazole: a review of its use in the management of superficial mycoses in dermatology and gynaecology. Drugs. 2009;69(3):339-59. doi: 10.2165/00003495-200969030-00009. 11(4):347-58. doi: 10.1586/eri.13.17.

    合成参考文献


    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
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