CAS: 848136-41-4; 4-[[3-(4-Acetylpiperazine-1-Carbonyl)-4-Fluorophenyl]Methyl]-2H-Phthalazin-1-One

该化合物是一种化学化合物,它与治疗用于癌症治疗的奥拉帕里布的药物发展有关,特别是治疗某些种类的乳腺癌和卵巢癌的药物,作为一种杂质,它通常是合成奥拉帕里布的副产品,在制造过程中可能出现.该化合物的特性可包括其分子结构,它可能与母体的奥拉帕里布化合物有关,其物理特性,如溶性,熔点和各种条件下的稳定性等.奥拉帕里布58等杂质在药物发展过程中很重要,对于确定药品发展的特点,以确保最终药物产品的安全性,功效和质量十分重要.通常使用HPLC,NMR和质量光谱分析技术来查明和量化此类杂质.了解杂质的特性对于遵守法规和维持药物配方的完整性至关重要.

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    上下游产品

    2-fluoro-5-[(4'-oxo-3'H-phthalazin-1'-yl)methyl]benzoic acid N-acetylpiperidine

    合成工艺路线路线简述

      📜5-[(3,4-二氢-4-氧代-1-酞嗪基)甲基]-2-氟苯甲酸,1-乙酰哌嗪置于o-(1H-Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Hexafluorophosphate,N,N-二异丙基乙胺体系中,用 N,N-二甲基乙酰胺 作为反应溶剂,化学反应生成 奥拉帕尼杂质58
      参考文献:4-[3-(4-Cyclopropanecarbonylpiperazine-1-Carbonyl)-4-Fluorobenzyl]-2H-Phthalazin-1-One: A Novel Bioavailable Inhibitor Of Poly(Adp-Ribose) Polymerase-1
      标题:4-[3-(4-Cyclopropanecarbonylpiperazine-1-Carbonyl)-4-Fluorobenzyl]-2H-Phthalazin-1-One: A Novel Bioavailable Inhibitor Of Poly(Adp-Ribose) Polymerase-1
      摘要:Poly(Adp-Ribose) Polymerase Activation Is An Immediate Cellular Response To Metabolic-,Chemical-,Or Ionizing Radiation-Induced Dna Damage And Represents A New Target For Cancer Therapy. In This Article,We Disclose A Novel Series Of Substituted 4-Benzyl-2H-Phthalazin-1-Ones That Possess High Inhibitory Enzyme And Cellular Potency For Both Parp-1 And Parp-2. Optimized Compounds From The Series Also Demonstrate Good Pharmacokinetic Profiles,Oral Bioavailability,And Activity In Vivo In An Sw620 Colorectal Cancer Xenograft Model. 4-[3-(4-Cyclopropanecarbonylpiperazine-1-Carbonyl)-4-Fluorobenzyl]-2H-Phthalazin-1-One (Ku-0059436,Azd2281) 47 Is A Single Digit Nanomolar Inhibitor Of Both Parp-1 And Parp-2 That Shows Standalone Activity Against Brca1-Deficient Breast Cancer Cell Lines. Compound 47 Is Currently Undergoing Clinical Development For The Treatment Of Brca1-And Brca2-Defective Cancers.
      DOI:10.1021/jm8001263

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      参考文献:10.1021/jm8001263
      摘要:Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S, Javaid H, Kerrigan F, Knights C, Lau A, Loh VM, Matthews IT, Moore S, O'Connor MJ, Smith GC, Martin NM. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581–91. doi: 10.1021/jm8001263.
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