CAS: 182760-06-1; 4-(2-((2R,3R)-3-(2,4-Difluorophenyl)-3-Hydroxy-4-(1H-1,2,4-Triazol-1-yl)Butan-2-yl)Thiazol-4-yl)Benzonitrile

该化合物是一种属于三甲醇类的抗风药剂,专门用来抑制对真菌细胞膜膜中雌性激素合成至关重要的14-demothyase,对真菌细胞膜膜中雌激素合成至关重要.这一行动机制使它能够有效防治广泛的真菌病原体,包括造成系统感染的病原体.Ravuconazole的特点是口服生物利用率高,而且具有有利的药源特性,从而能够以较不经常的剂量来有效治疗.它表现出一种良好的安全性能,通常具有轻度和可管理的不利影响.该化合物还明显地表明它有可能用于治疗各种真菌感染,包括耐其他抗菌剂的物种.它的化学结构包括一个三角菌环,有助于它的活动和稳定.Ravuconazole的发育反映了加强抗风药疗法的持续努力,特别是在菌原病原体抗药抗力日益增强的情况下.

结构式图片

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上下游产品

CAS号20099-89-2 2-溴-4'-氰基苯乙酮 | CAS号170863-34-0 (2R,3R)-3-(2,4-... | CAS号1443-80-7 4-乙酰基苯甲腈 | CAS号170862-36-9 (αS,βR)-β-(2,4-...

合成工艺路线路线简述

  • 合成目标产物 Ravuconazole 主要起始原料 4-Acetylbenzonitrile
  • (文献来源)合成步骤主要原料 4-Acetylbenzonitrile
📜(2R,3R)-3-[4-(4-Cyanophenyl)Thiazol-2-Yl]-1-(1H-1,2,4-Triazol-1-yl)-2-(2,4-Difluorophenyl)-Butan-2-Ol (1R)-10-Camphorsulfonate置于sodium Hydroxide体系中,用 二氯甲烷,水 用作溶剂,化学反应生成雷夫康唑
参考文献:Process For The Manufacture Of Enantiomerically Pure Antifungal Azoles As Ravuconazole And Isavuconazole
标题:Process For The Manufacture Of Enantiomerically Pure Antifungal Azoles As Ravuconazole And Isavuconazole
摘要:一种新的技术过程,通过拆分外消旋体来制备公式i的对映纯抗真菌化合物已被披露.

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: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-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.

专利号:US-12325678-B2
优先权日:2017-06-16
标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
发明人:OJIMA IWAO; DEL POETA MAURIZIO; LAZZARINI CRISTINA; HARANAHALLI KRUPANANDAN; SUN YI
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present invention provides a compound having the structure: n nand use of the compound for inhibiting the growth of or killing.

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

专利号:US-11858880-B2
优先权日:2017-06-16
标题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids

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主要参考文献


1: Tsunemi Y, Naka W. Exploratory study on short-term administration of oral fosravuconazole for tinea pedis. J Dermatol. 2024 Sep 10. doi: 10.1111/1346-8138.17455. Epub ahead of print.
57:e00411. doi: 10.1590/0037-8682-0585-2023.
3: Deng X, Song CC, Gu WJ, Wang YJ, Feng L, Zhou XJ, Zhou MQ, Yuan WC, Chen YZ. Regioselective and enantioselective propargylic hydroxylations catalyzed by P450tol monooxygenases. Bioresour Bioprocess. 2024 Jul 2;11(1):64. doi: 10.1186/s40643-024-00771-7.

合成参考文献


参考文献:10.1007/bf02752281
摘要:Abuhammour W, Habte-Gabr E. Systemic antifungal agents. Indian J Pediatr. 2001 Jul;68(7):655–68. doi: 10.1007/bf02752281.
参考文献:10.1128/jcm.39.9.3254-3259.2001
摘要:Pfaller MA, Diekema DJ, Jones RN, Sader HS, Fluit AC, Hollis RJ, Messer SA; SENTRY Participant Group. International surveillance of bloodstream infections due to Candida species: frequency of occurrence and in vitro susceptibilities to fluconazole, ravuconazole, and voriconazole of isolates collected from 1997 through 1999 in the SENTRY antimicrobial surveillance program. J Clin Microbiol. 2001 Sep;39(9):3254–9.
参考文献:10.1007/978-0-387-77570-8_6
摘要:Buckner FS. Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections. Adv Exp Med Biol. 2008;625():61–80. doi: 10.1007/978-0-387-77570-8_6.
参考文献:10.1186/1752-1947-5-205
摘要:Banerji JS, Singh J C. Cutaneous Fusarium infection in a renal transplant recipient: a case report. Journal of Medical Case Reports. 2011 May 25;5(1):205. doi: 10.1186/1752-1947-5-205.
参考文献:10.1007/bf03256665
摘要:Feldmesser M. New and emerging antifungal agents: impact on respiratory infections. Am J Respir Med. 2003;2(5):371–83. doi: 10.1007/bf03256665.
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