CAS: 1393477-72-9; (Z)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)-N'-(Pyrazin-2-yl)Acrylohydrazide

该化合物是一个小分子抑制剂,主要针对出口的1(XPO1)蛋白质,该蛋白质在各种肿瘤抑制蛋白的核出口中起着关键作用,该化合物被归类为抗肾塑料剂,主要用于治疗某些类型的癌症,特别是多种间皮瘤和大B细胞淋巴瘤的传播.Selinexor因能够防止核心的亲食性因素输出,从而在癌症细胞中诱发流感.该物质通常通过口服方式施用,并拥有与传统化疗剂相比独特的行动机制.其功效往往与其他疗法结合评估,以提高治疗结果.Selineor的副作用可能包括疲劳,恶心和细胞细胞癌,这在癌症治疗中很常见.作为一种有针对性的疗法,它代表了癌症治疗方法的一大进步,重点是肿瘤生长和存活过程中的分子途径.

结构式图片

上下游产品

3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazole (Z)-isopropyl 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid 2-hydrazinylpyrazine

合成工艺路线路线简述

  • 合成目标产物 Kpt-330 主要起始原料 (Z)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)Acrylic Acid And 2-Hydrazinopyrazine
  • (文献来源)合成步骤主要原料 (Z)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)Acrylic Acid 和 2-Hydrazinopyrazine
3-(3,5-双(三氟甲基)苯基)-1H-1,2,4-三唑置于水,Potassium Carbonate,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,Lithium Hydroxide体系中,用 四氢呋喃,甲醇,乙酸乙酯,乙腈 用作溶剂,化学反应 9.75H,反应生成塞利尼索
参考文献: Novel Crystalline Forms Of Selinexor And Process For Their Preparation[fr] Nouvelles Formes Cristallines De Sélinexor Et Leur Procédé De Préparation
标题: Novel Crystalline Forms Of Selinexor And Process For Their Preparation[fr] Nouvelles Formes Cristallines De Sélinexor Et Leur Procédé De Préparation
摘要:本公开涉及selinexor的固态形式,其制备过程以及其制备的制药组合物.

海关参考信息

专利信息


专利号:US-2018297925-A1
优先权日:2015-10-12
标题 :Methods for total synthesis of resolvin e1
发明人:JAGTAP PRAKASH
权利人:SALZMAN LOVELACE INVEST LTD
摘要:Methods for total chemical synthesis of Resolvin E1 (RvE1) include Wittig reaction of two compounds having hydroxyl protecting group in the presence of a strong base, removal of the hydroxyl-protecting groups with a deprotecting reagent to produce a compound having an ester group, and hydrolysis of the ester group to obtain RvE1

专利号:US-6262251-B1
优先权日:1995-10-19
标题 :Method for solution phase synthesis of oligonucleotides
发明人:PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING
权利人:PROLIGO LLC
摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides. The method lends itself to automation and is ideally suited for large scale manufacture of oligonucleotides with high efficiency.

专利号:EP-1501848-B1
优先权日:2002-05-08
标 题 :Synthesis of locked nucleic acid derivatives
发明人:SORENSEN MADS DETLEF; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER
权利人:SANTARIS PHARMA AS
摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as alpha-L-oxy-LNA, amino-LNA, alpha-L-amino-LNA, thio-LNA, alpha-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. (Formula I)

专利号:US-5874532-A
优先权日:1997-01-08
标 题 :Method for solution phase synthesis of oligonucleotides and peptides
发明人:PIEKEN WOLFGANG; GOLD LARRY
权利人:NEXSTAR PHARMACEUTICALS INC
摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides and peptides. The method lends itself to automation and is ideally suited for large scale manufacture oligonucleotides with high efficiency.

专利号:EP-1383732-B1
优先权日:2001-05-04
标题:Labelling reagents, method for synthesis of said reagents and methods for detecting biological molecules
发明人:BOURGET CECILE; LHOMME JEAN; LAAYOUN ALI; KOTERA MITSUHARU; TREVISIOL EMMANUELLE; MENOU LIONEL; BERNAL MENDEZ ELOY
权利人:BIO MERIEUX; UNIV GRENOBLE 1; CENTRE NAT RECH SCIENT
摘要:The invention concerns a temperature-stable labelling reagent of formula (I), wherein: R<1> represents H or an alkyl, aryl or substituted aryl group; R<2> represents a detectable marker or at least two detectable markers linked together by at least a multimeric structure; L is a linking arm comprising a linear catemer concatenation of at least two covalent bonds; and n is an integer equal to 0 or 1; R<3> and R<4> represent, independently of each other: H, NO2, Cl, Br, F, I, R<2>-(L)n-Y-X-, OR, SR, NR2, R, NHCOR, CONHR, COOR with R = alkyl or aryl, A is a linking arm comprising at least a double bond enabling the conjugation of the diazo function with the aromatic cycle; and u is a whole number between 0 and 2, preferably between 0 and 1; and -Y-X- represents -CONH-, -NHCO-, -CH2O-, -CH2S-. The invention also concerns a method for the synthesis of said markers and uses for labelling biological molecules, in particular nucleic acids, with a labelling reagent bearing the diazomethyl function. The invention is particularly applicable in the field of diagnosis.

专利号:US-6001966-A
优先权日:1995-10-19
标题 :Method for solution phase synthesis of oligonucleotides and peptides
发明人:PIEKEN WOLFGANG; GOLD LARRY
权利人:PROLIGO LLC
摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides and peptides. The method lends itself to automation and is ideally suited for large scale manufacture oligonucleotides with high efficiency.
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主要参考文献


1: Wang AY, Weiner H, Green M, Chang H, Fulton N, Larson RA, Odenike O, Artz AS, Bishop MR, Godley LA, Thirman MJ, Kosuri S, Churpek JE, Curran E, Pettit K, Stock W, Liu H. A phase I study of selinexor in combination with high-dose cytarabine and mitoxantrone for remission induction in patients with acute myeloid leukemia. J Hematol Oncol. 2018 Jan 5;11(1):4. doi: 10.1186/s13045-017-0550-8. doi: 10.18632/oncotarget.22801. eCollection 2017 Dec 15.
3: Chim CS, Kumar SK, Orlowski RZ, Cook G, Richardson PG, Gertz MA, Giralt S, Mateos MV, Leleu X, Anderson KC. Management of relapsed and refractory multiple myeloma: novel agents, antibodies, immunotherapies and beyond. Leukemia. 2017 Jan 16. doi: 10.1038/leu.2017.329. [Epub ahead of print] Review. doi: 10.1016/j.bcp.2017.11.009. Epub 2017 Nov 16. doi: 10.18632/oncotarget.19285. eCollection 2017 Oct 10.
8: Chen Y, Zhang L, Huang J, Hong X, Zhao J, Wang Z, Zhang K. Dasatinib and chemotherapy in a patient with early T-cell precursor acute lymphoblastic leukemia and NUP214-ABL1 fusion: A case report. Exp Ther Med. 2017 Nov;14(5):3979-3984. doi: 10.3892/etm.2017.5046. Epub 2017 Aug 28.

合成参考文献


摘要:Liu, G.; Feng, J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 325.
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