CAS: 2101700-15-4; (S)-5-Amino-3-(4-((5-Fluoro-2-Methoxybenzamido)Methyl)Phenyl)-1-(1,1,1-Trifluoropropan-2-yl)-1H-Pyrazole-4-Carboxamide
- 英文名称(S)-5-Amino-3-(4-((5-Fluoro-2-Methoxybenzamido)Methyl)Phenyl)-1-(1,1,1-Trifluoropropan-2-yl)-1H-Pyrazole-4-Carboxamide
- 中文名称5-氨基-3-[4-[(5-氟-2-甲氧基苯甲酰基)氨基]甲基]苯基]-1-[(1S)-2,2,2-三氟-1-甲基乙基]-1H-吡唑-4-甲酰胺
- IUPAC名称(S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide
- 其它别名(S)-5-Amino-3-(4-((5-Fluoro-2-Methoxybenzamido)Methyl)Phenyl)-1-(1,1,1-Trifluoropropan-2-yl)-1H-Pyrazole-4-Carboxamide; 1H-Pyrazole-4-Carboxamide, 5-Amino-3-[4-[[(5-Fluoro-2-Methoxybenzoyl)Amino]Methyl]Phenyl]-1-[(1S)-2,2,2-Trifluoro-1-Methylethyl]-; Lo
- CAS编号2101700-15-4
- MFCD编号:MFCD34179491
- EINECS号:864-730-9
- FDA UNII编号:JNA39I7ZVB
- 分子式:C22H21F4N5O3
- 分子量:479.43
- 产品CID: 1086986
- 同类组份化合物CAS2101700-15-4 (S-isomer)2101700-14-3 (R-isomer)
- 产品分类医药中间体
物理性质
- 沸点619.2±55.0 °C(预测)
- 密度1.44±0.1 g/cm3(预测)
- pKa:13.32±0.46(预测)
- LogP:3.3
- 溶解性DMSO: 50 mg/mL (104.29 Mm; Need Ultrasonic)
- 外观形态白色至黄色固体
- 储存条件4°C, 氮气保护
- 产品应用该化合物用作治疗患有复发或复发性曼体淋巴瘤(MCL)的成年病人的口服,选择性强,非COVALENT BRUZTON的强性性脊髓炎抑制剂(BTK),这些病人已经接受过前期治疗,包括共价的BT K抑制剂 (例如IBRUTINIB) 和至少两行系统治疗;它还被批准治疗慢性淋巴细胞白血病(CLL)和小淋巴性淋巴眼(SLL);它显示出对抗野型和C481-变型BTK的功效,克服了与共价BT-K抑制剂相关的抗药性,抑制了B细胞受体信号,从而抑制了 B细胞和子细胞的扩散和生存.
MSDS等安全信息
欧盟法规
C&L通报合成工艺路线路线简述
5-氟-2-甲氧基苯甲酰氯置于甲烷磺酸,水,溶剂黄146,三乙胺,N,N-二异丙基乙胺体系中,用 乙醇,二氯甲烷 用作溶剂,化学反应 22.0H,反应生成5-氨基-3-[4-[(5-氟-2-甲氧基苯甲酰基)氨基]甲基]苯基]-1-[(1S)-2,2,2-三氟-1-甲基乙基]-1H-吡唑-4-甲酰胺
参考文献:一种淋巴瘤治疗药物中间体的制备方法
标题:一种淋巴瘤治疗药物中间体的制备方法
摘要:本发明公开了一种淋巴瘤治疗药物吡托布鲁替尼中间体的制备方法:步骤1,4‑氨基甲基苯甲酸与丙二腈反应,得到中间体2‑(4‑(氨基甲基)苯甲酰基)丙二腈;步骤2,步骤产物发生酰胺化反应得到中间体n‑(4‑(2,2‑二氰基乙酰基)苄基)‑5‑氟‑2‑甲氧基苯甲酰胺;步骤3,步骤2产物与[(Ls)‑2,2,2‑三氟‑1‑甲基‑乙基]盐酸肼发生环合反应得到n‑[[4‑[(Ls)‑5‑胺基‑4‑氰基‑1‑(2,2,2‑三氟‑1‑甲基‑乙基)吡唑‑3‑基]苯基]甲基]‑5‑氟‑2‑甲氧基‑苯甲酰胺.本发明所述吡托布鲁替尼中间体的合成方法,相对现有技术优势明显,路线短,高收率,环境友好,副产物较少.
海关参考信息
- 2905110000-甲醇
2912110000-甲醛
2912210000-苯甲醛
2907121100-间甲酚 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
专利号:WO-2025137620-A1
优先权日:2023-12-21
标题:Methods for high quality and high accuracy methylation sequencing
发明人：KENNEDY ANDREW
权利人:GUARDANT HEALTH INC
摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.
专利号:CN-118063341-A
优先权日:2024-02-21
标 题 :Synthesis method of pitobutinib intermediate
专利号:CN-119059973-A
优先权日:2024-08-12
标题:Pituo cloth Synthesis process of rutinib
专利号:CN-119059972-A
优先权日:2024-08-12
标题:Synthesis method of BTK inhibitor pirtobuttinib
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Gomez EB, Ebata K, Randeria HS, Rosendahl MS, Cedervall EP, Morales TH, Hanson LM, Brown NE, Gong X, Stephens J, Wu W, Lippincott I, Ku KS, Walgren RA, Abada PB, Ballard JA, Allerston CK, Brandhuber BJ. Preclinical characterization of pirtobrutinib, a highly selective, noncovalent (reversible) BTK inhibitor. Blood. 2023 Jul 6;142(1):62-72. doi: 10.1182/blood.2022018674.
2: Mato AR, Shah NN, Jurczak W, Cheah CY, Pagel JM, Woyach JA, Fakhri B, Eyre TA, Lamanna N, Patel MR, Alencar A, Lech-Maranda E, Wierda WG, Coombs CC, Gerson JN, Ghia P, Le Gouill S, Lewis DJ, Sundaram S, Cohen JB, Flinn IW, Tam CS, Barve MA, Kuss B, Taylor J, Abdel-Wahab O, Schuster SJ, Palomba ML, Lewis KL, Roeker LE, Davids MS, Tan XN, Fenske TS, Wallin J, Tsai DE, Ku NC, Zhu E, Chen J, Yin M, Nair B, Ebata K, Marella N, Brown JR, Wang M. Pirtobrutinib in relapsed or refractory B-cell malignancies (BRUIN): a phase 1/2 study. Lancet. 2021 Mar 6;397(10277):892-901. doi: 10.1016/S0140-6736(21)00224-5.
3: Wang ML, Jurczak W, Zinzani PL, Eyre TA, Cheah CY, Ujjani CS, Koh Y, Izutsu K, Gerson JN, Flinn I, Tessoulin B, Alencar AJ, Ma S, Lewis D, Lech-Maranda E, Rhodes J, Patel K, Maddocks K, Lamanna N, Wang Y, Tam CS, Munir T, Nagai H, Hernandez-Ilizaliturri F, Kumar A, Fenske TS, Seymour JF, Zelenetz AD, Nair B, Tsai DE, Balbas M, Walgren RA, Abada P, Wang C, Zhao J, Mato AR, Shah NN. Pirtobrutinib in Covalent Bruton Tyrosine Kinase Inhibitor Pretreated Mantle- Cell Lymphoma. J Clin Oncol. 2023 Aug 20;41(24):3988-3997. doi: 10.1200/JCO.23.00562. Epub 2023 May 16.
合成参考文献
摘要:FDA label
📝 需求与反馈
尽可能描述清楚需求与问题信息
