CAS: 927880-90-8; 1-Methyl-5-((2-(5-(Trifluoromethyl)-1H-Imidazol-2-yl)Pyridin-4-yl)Oxy)-N-(4-(Trifluoromethyl)Phenyl)-1H-Benzo[d]Imidazol-2-Amine

该化合物是一个化学化合物,在医学化学领域引起注意,特别是其作为治疗剂的潜力,被归类为小分子抑制剂,具体针对细胞信号传输路径中涉及的某些动脉酶;复合物具有可能有助于治疗各种疾病包括癌症的功效的特性;RAF 265, 因其有能力抑制在MAPK/ERK信号路径中起关键作用的亚麻风家族的活动,经常与肿瘤产生有关;就其物理特征而言,RAF 265通常在室温上呈固态,具有与药物应用配方相关的具体溶性和稳定性特征;其开发工作是正在进行的研究的一部分,旨在了解其药代物学,生物可用性和总体治疗潜力;与许多调查性化合物一样,进一步的研究对于充分阐明其在临床环境中的安全性和有效性至关重要.

结构式图片

物理性质

MSDS等安全信息

上下游产品

1-methyl-4-((2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yl)oxy)benzene-1,2-diamineN1-methyl-4-((2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yl)oxy)benzene-1,2-diamine 4-(trifluoromethyl)phenyl isothi°Cyanate 3-bromo-1,1,1-trifluoroacetone tert-butyl 4-(4-(methylamino)-3-nitrophenoxy)picolinate2-{4-[1-methyl-2-(4-trifluoromethyl-phenylamino)-1H-benzoimidazol-5-yloxy]-pyridin-2-yl}-3H-imidazole-4-carbonitrile

合成工艺路线路线简述

  • 合成目标产物 Raf265(Chir-265) 主要起始原料 1,2-Benzenediamine, N1-Methyl-4-[[2-[5-(Trifluoromethyl)-1H-Imidazol-2-Yl]-4-Pyridinyl]Oxy]- And 4-(Trifluoromethyl)Phenyl Isothiocyanate
  • 1645-65-4 + 927880-89-5 = 927880-90-8
    反应条件:1.1 Solvents: Methanol; 16 H,Rt1.2 Reagents: Iron Chloride (Fecl3) Solvents: Methanol; Overnight,Rt
    标题:Discovery Of Raf265: A Potent Mut-B-Raf Inhibitor For The Treatment Of Metastatic Melanoma
    作者:Williams,Teresa E.; Subramanian,Sharadha; Verhagen,Joelle; Mcbride,Christopher M.; Costales,Abran; Et Al
    参考文献:Acs Medicinal Chemistry Letters 日期:2015 卷标:6(9) 页码:961-965]

    1645-65-4 + 927880-89-5 = 927880-90-8
    反应条件:1.1 Solvents: Methanol; Rt; 16 H,Rt1.2 Reagents: Iron Chloride (Fecl3) Solvents: Methanol; Overnight,Rt
    标题:Preparation Of Forms A-P Of 1-Methyl-5-[2-(5-Trifluoromethyl-1H-Imidazol-2-Yl)Pyridin-4-Yloxy]-N-(4-Trifluoromethylphenyl)-1H-Benzo[d]Imidazol-2-Amine Having Specified X-Ray Powder Diffraction Patterns As Raf Kinase Inhibitors.
    参考文献:World Intellectual Property Organization]

    1645-65-4 + 927880-89-5 = 927880-90-8
    反应条件:1.1 Solvents: Methanol; 16 H,Rt1.2 Reagents: Iron Chloride (Fecl3) Solvents: Methanol; Overnight,Rt1.3 Reagents: Sodium Carbonate Solvents: Water; Ph 10
    标题:Formulations For Benzimidazolyl Pyridyl Ethers
    参考文献:World Intellectual Property Organization]

    1645-65-4 + 927880-89-5 = 927880-90-8
    反应条件:1.1 Solvents: Acetonitrile; 20 Min,Rt1.2 Reagents: Triethylamine,2-Chloro-1-Methylpyridinium Iodide; Rt; 5 H,Rt -> 50 °C
    标题:Method For The Preparation Of Benzimidazoles
    参考文献:United States]

    = 927880-90-8 [标题:Reaction Conditions
    标题:Formulations For Benzimidazolyl Pyridyl Ethers
    参考文献:United States]

    = 927880-90-8 [标题:Reaction Conditions
    标题:Solid Forms Of A Raf Kinase Inhibitor
    参考文献:United States]

    = 927880-90-8 [标题:Reaction Conditions
    标题:Salts Of Benzimidazolyl Pyridyl Ethers And Formulations Thereof For Cancer Treatment
    参考文献:World Intellectual Property Organization
📜4-氯吡啶-2-羧酸叔丁酯置于manganese(Iv) Oxide,Lithium Aluminium Tetrahydride,Sodium Dithionite,氨,水,Sodium Carbonate,Potassium Carbonate,三氟乙酸酐体系中,用 四氢呋喃,甲醇,乙醇,二氯甲烷,氯仿,水,二甲基亚砜,乙腈 作为反应溶剂,化学反应 117.0H,反应生成 1-甲基-5-[[2-[5-(三氟甲基)-1H-咪唑-2-基]-4-吡啶基]氧基]-N-[4-(三氟甲基)苯基]-1H-苯并咪唑-2-胺
参考文献:Wo2008/140850
标题:Wo2008/140850

海关参考信息

专利信息


专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人：SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.

专利号:CN-117624129-A
优先权日:2023-10-17
标题:A kind of RAF265 inhibitor synthesis method

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主要参考文献


1: Rajadurai A, Tsao H. Identification of Collagen-Suppressive Agents in Keloidal Fibroblasts Using a High-Content, Phenotype-Based Drug Screen. JID Innov. 2023 Nov 22;4(2):100248. doi: 10.1016/j.xjidi.2023.100248.
2: Ercoli MF, Ramos PZ, Jain R, Pilotte J, Dong OX, Thompson T, Wells CI, Elkins JM, Edwards AM, Couñago RM, Drewry DH, Ronald PC. An open source plant kinase chemogenomics set. Plant Direct. 2022 Nov 25;6(11):e460. doi: 10.1002/pld3.460.
3: Wang J, Tian WJ, Li CC, Zhang XZ, Fan K, Li SL, Wang XJ. Small-Molecule RAF265 as an Antiviral Therapy Acts against PEDV Infection. Viruses. 2022 Oct 15;14(10):2261. doi: 10.3390/v14102261.

合成参考文献


参考文献:10.1007/s11302-008-9111-5
摘要:García-Echeverría C. Protein and lipid kinase inhibitors as targeted anticancer agents of the Ras/Raf/MEK and PI3K/PKB pathways. Purinergic Signalling. 2008 Jun 04;5(1):117–25. doi: 10.1007/s11302-008-9111-5.
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