CAS: 1557267-42-1; N-(3-((2-((3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenyl)Amino)-7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Oxy)Phenyl)Acrylamide
- 英文名称N-(3-((2-((3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenyl)Amino)-7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Oxy)Phenyl)Acrylamide
- 中文名称艾维替尼
- IUPAC名称N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide
- 其它别名Abivertinib; Abivertinib [inn]; N-(3-((2-((3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenyl)Amino)-7H-Pyrrolo(2,3-D)Pyrimidin-4-yl)Oxy)Phenyl)Prop-2-Enamide; N-[3-[[2-[[3-Fluoro-4-(4-Methyl-1-Pi
- CAS编号1557267-42-1
- MFCD编号:MFCD29089376
- FDA UNII编号:CER0OPG92L
- 分子式:C26H26FN7O2分子量:487.54
- 产品CID: 773240
- 同类组份化合物CAS1557267-42-1 (free base)1557268-88-8 (maleate)1822357-78-7 (maleate hydrate)1557268-90-2 (2HCl)1801879-16-2 (HCl)
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
- 密度1.4±0.1 g/cm3
- pKa:12.48±0.50(预测)
- LogP:3.5
- 折射率1.697
- 溶解性DMSO:30.0(Max Conc. mg/mL);61.53(Max Conc. Mm)
- 外观形态白色至类白色结晶性固体
- 储存条件储存在 -20°C
- 产品应用该化合物是一种不可逆的EGFR抑制器,对变异的EGBFR(特别是EG FR L858R/T790M双变异体(IC50=0.18 NM),其威力比野型EGRFR (IC50 = 7.68 NM) 高约43倍.它显示出抗突触活动,有利于耐受性.AVITINIB 有效地在使用口服时(超过143天,每天500毫克/千克/天),在预留启动EGVFR和T7900M突变的化学模型中,引发了完全的肿瘤回归.它表明,NCI-H1975和NIH/3T3-TC332T8细胞(分别为IC50和7.3 NM和2.8 NM,分别是431细胞中野型 EGFFRER的威力,其选择率为115至298倍.此外,它禁止下游效应器AKT和ERK1/2的磷化作用.
上下游产品
N-(3-(2-(3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenylamino)-7-(Hydroxymethyl)-7H-Pyrrolo[2,3-D]Pyrimidin-4-Yloxy)Phenyl)Acrylamide 1557267-50-1N-(3-(2-(3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenylamino)-7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidin-4-Yloxy)Phenyl)Acrylamide 1557268-64-0
4-(3-Aminophenoxy)-N-(3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenyl)-7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidin-2-Amine 1557268-61-7
N-(3-Fluoro-4- (4-Methylpiperazin-1-yl)Phenyl)-4-(3-Nitrophenoxy)-7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidin-2-Amine 1557268-58-2
(2-Chloro-4-(3-Nitrophenoxy)-7H-Pyrrolo[2,3-D]Pyrimidin-7-yl)Methyl Pivalate 1557268-80-0
2-Chloro-4-(3-Nitrophenoxy)-7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidine 1557268-35-5
合成工艺路线路线简述
📜N-(3-(2-(3-Fluoro-4-(4-Methylpiperazin-1-yl)Phenylamino)-7-(Hydroxymethyl)-7H-Pyrrolo[2,3-D]Pyrimidin-4-Yloxy)Phenyl)Acrylamide置于乙醇,Potassium Carbonate体系中,化学反应 4.0H,以86.7%的收率获得艾维替尼
参考文献:艾维替尼的新合成路线及其马来酸盐二水合物
标题:艾维替尼的新合成路线及其马来酸盐二水合物
摘要:本发明公开了艾维替尼的一种新合成工艺,以2‑氯‑4‑(3‑硝基苯氧基)‑7氢‑(吡咯并[2,3‑d]嘧啶)‑1‑甲基叔丁酸酯为起始原料,反应路线短,总产率高;脱保护基更加容易,后处理简单,在规模化生产中具有重要的应用价值.本发明还涉及马来酸盐二水合物及其优选晶型,具有优异的粉末特性,特别有利于固体制剂加工,特别是制成胶囊剂.最后,本发明还公开了以马来酸盐二水合物为活性成分的胶囊剂,内容物的流动性非常好,释放度达到药典标准.
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2912110000-甲醛
2912120000-乙醛 - 💡 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-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.
供应商参考报价(招募中)
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: Huang J, Huang X, Li Y, Li X, Wang J, Li F, Yan X, Wang H, Wang Y, Lin X, Tu J, He D, Ye W, Yang M, Jin J. Abivertinib inhibits megakaryocyte differentiation and platelet biogenesis. Front Med. 2022 Jun;16(3):416-428. doi: 10.1007/s11684-021-0838-5. Epub 2021 Nov 18. 59(5):90. doi: 10.3892/ijo.2021.5270. Epub 2021 Sep 24.
3: Wang H, Pan R, Zhang X, Si X, Wang M, Zhang L. Abivertinib in patients with T790M-positive advanced NSCLC and its subsequent treatment with osimertinib. Thorac Cancer. 2020 Mar;11(3):594-602. doi: 10.1111/1759-7714.13302. Epub 2020 Jan 14.
4: Nagasaka M, Zhu VW, Lim SM, Greco M, Wu F, Ou SI. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763. doi: 10.1016/j.jtho.2020.11.028. Epub 2020 Dec 15. 14(10):2560-2573. doi: 10.1002/1878-0261.12742. Epub 2020 Jul 3.
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