CAS: 1642300-52-4; (E)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)-2-(Pyrimidin-5-yl)Acrylamide

📜3,5-双三氟甲基苯腈置于n-甲基吗啉,三乙烯二胺,Sodium Hydrogen Sulfide,Bis-Triphenylphosphine-Palladium(II) Chloride,Hydrazine Hydrate,Lithium Hydroxide Monohydrate,水,溴,Sodium Acetate,三乙胺,Magnesium Chloride,氯甲酸异丁酯体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 27.0H,反应生成艾他尼索
参考文献:一种氮唑类衍生物或其药物可接受盐及其制备方法和用途
标题:一种氮唑类衍生物或其药物可接受盐及其制备方法和用途
摘要:本发明公开了一种氮唑类衍生物或其药物可接受盐及其制备方法,所述氮唑类衍生物结构如下所示,与现有技术相比,本发明供一种结构新颖的且具有抑制crm1蛋白功能的氮唑类化合物,它们作为crm1蛋白抑制剂,能阻断肿瘤细胞增殖,诱发肿瘤细胞凋亡,从而可用于人和动物的多种疾病如恶性肿瘤的治疗和预防,效果显著更优.

专利信息

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:WO-2022246227-A1
优先权日:2021-05-20
标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:CA-3219525-A1
优先权日:2021-05-20
标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:EP-4341253-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms