CAS: 1092364-38-9; 1-(4-((4-((3,4-Dichloro-2-Fluorophenyl)Amino)-7-Methoxyquinazolin-6-yl)Oxy)Piperidin-1-yl)Prop-2-En-1-One

该化合物是一种主要为治疗某些类型癌症,特别是非小型细胞肺癌(NSCLC)而研制的微小分子气压强性激素性激素抑制剂,有选择性地针对上皮生长因子受体(EGFR)和人类上皮生长因子受体2(HER2),后者经常与肿瘤的生长和扩散有关;该化合物的特征是它能够抑制这些受体的野性形式和变异形式,使它成为抵抗其他治疗的病人的潜在治疗选择;Poziotinib通常通过口服,并在临床试验中评估其功效和安全特征;其化学结构包括一种五氯硝基苯核心,在许多动脉抑制剂中很常见,并显示出能够有效地与目标受体相连的特性;与许多有针对性的疗法一样,在治疗期间,监测副作用和药物相互作用至关重要;

结构式图片

上下游产品

4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-ol 1-acryloylpiperidin-4-yl 4-methylbenzenesulfonate 1-(3-chloropropanoyl)piperidin-4-yl 4-methylbenzenesulfonate 6-acetoxy-7-methoxy-3,4-dihydroquinazolin-4-one1-[4-[4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy]-piperidin-1-yl]prop-2-en-1-one hydr°Chloride

合成工艺路线路线简述

  • 合成目标产物 Poziotinib (Hm781-36B) 主要起始原料 4-(3,4-Dichloro-2-Fluorophenylamino)-7-Methoxyquinazolin-6-Ol And 1-[4-[[(4-Methylphenyl)Sulfonyl]Oxy]-1-Piperidinyl]-2-Propen-1-One
  • (文献来源)合成步骤主要原料 4-(3,4-Dichloro-2-Fluorophenylamino)-7-Methoxyquinazolin-6-Ol 和 1-[4-[[(4-Methylphenyl)Sulfonyl]Oxy]-1-Piperidinyl]-2-Propen-1-One
📜3,4-二氯-2-氟苯胺置于氨,Potassium Carbonate,N,N-二异丙基乙胺,三氯氧磷体系中,用 甲醇,N,N-二甲基乙酰胺,甲苯 用作溶剂,化学反应 29.33H,反应生成波齐替尼
参考文献: Method For Preparing 1-(4-(4-(3,4-Dichloro-2-Fluorophenylamino)-7-Methoxyquinazolin-6-Yloxy)Piperidin-1-yl)Prop-2-En-1-One[fr] Procédé De Préparation De 1-(4-(4-(3,4-Dichloro-2-Fluorophénylamino)-7-Méthoxyquinazolin-6-Yloxy)Pipéridin-1-yl)Prop-2-én-1-One
标题: Method For Preparing 1-(4-(4-(3,4-Dichloro-2-Fluorophenylamino)-7-Methoxyquinazolin-6-Yloxy)Piperidin-1-yl)Prop-2-En-1-One[fr] Procédé De Préparation De 1-(4-(4-(3,4-Dichloro-2-Fluorophénylamino)-7-Méthoxyquinazolin-6-Yloxy)Pipéridin-1-yl)Prop-2-én-1-One
摘要:本发明涉及一种新型制备1-(4-(4-(3,4-二氯-2-氟苯胺基)-7-甲氧基喹唑啉-6-氧基)哌啶-1-基)丙-2-烯-1-酮的方法,与传统方法相比,通过允许4-(3,4-二氯-2-氟苯胺基)-7-甲氧基喹唑啉-6-醇与n-酰基哌啶衍生物在惰性极性质子溶剂中在碱的存在下反应,实现了更简单的工艺过程.

海关参考信息

专利信息


专利号:US-2022064145-A1
优先权日:2020-08-28
标 题 :Synthesis of poziotinib derivative
发明人:BANG KEUK CHAN; MOON YOUNG HO; CHANG YOUNG KIL
权利人:HANMI SCIENCE CO LTD
摘要:A method for the synthesis of a compound of Formula II is provided. Also disclosed is the salt form of the compound. The method includes the introduction of a piperidinyl moiety in a polar aprotic solvent system, followed by the removal of the protecting group and the acrylation step.

专利号:US-2021221792-A1
优先权日:2020-01-16
标题:Convergent synthesis of poziotinib derivative
发明人:CHAN BANG KEUK; HYUK JUNG JAE; HO MOON YOUNG
权利人:HANMI PHARM IND CO LTD
摘要:A method of for the synthesis of a compound of Formula I is disclosed herein. The method includes reacting a compound of formula (II) with a compound of formula (III) in an inert polar aprotic solvent system in the presence of a base.

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人:RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:WO-2022043923-A1
优先权日:2020-08-28
标题 :Synthesis of poziotinib derivative

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

✅ COA系统入驻 | 共享模式

主要参考文献


1: Park S, Park S, Kim TM, Kim S, Koh J, Lim J, Yi K, Yi B, Ju YS, Kim M, Keam B, Kim JS, Jeon YK, Kim DW, Kim YT, Heo DS. Resistance mechanisms of EGFR tyrosine kinase inhibitors, in EGFR exon 20 insertion-mutant lung cancer. Eur J Cancer. 2024 Jul 4;208:114206. doi: 10.1016/j.ejca.2024.114206. Epub ahead of print. 25(11):5917. doi: 10.3390/ijms25115917.
3: Park J, Lee B, Song JY, Sung M, Kwon MJ, Kim CR, Lee S, Shin YK, Choi YL. Detection of EGFR exon 20 insertion mutations in non-small cell lung cancer: implications for consistent nomenclature in precision medicine. Pathology. 2024 Aug;56(5):653-661. doi: 10.1016/j.pathol.2024.02.012. Epub 2024 May 6. 10(9):e30312. doi: 10.1016/j.heliyon.2024.e30312.
5: Ippolitov D, Lin YH, Spence J, Glogowska A, Thanasupawat T, Beiko J, Del Bigio MR, Xu X, Wang A, Calvo R, Kapoor A, Marugan JJ, Henderson MJ, Klonisch T, Hombach-Klonisch S. Overcoming brain-derived therapeutic resistance in HER2+ breast cancer brain metastasis. bioRxiv [Preprint]. 2024 Feb

合成参考文献


参考文献:10.1038/s41571-018-0038-7
摘要:Romero D. Poziotinib for uncommon ERBB mutations. Nature Reviews Clinical Oncology. 2018 May 09;15(7):404. doi: 10.1038/s41571-018-0038-7.
参考文献:10.1186/s12916-022-02245-z
摘要:Song Z, Li Y, Chen S, Ying S, Xu S, Huang J, Wu D, Lv D, Bei T, Liu S, Huang X, Xie C, Wu X, Fu J, Hua F, Wang W, Xu C, Gao C, Cai S, Lu S, Zhang Y. Efficacy and safety of pyrotinib in advanced lung adenocarcinoma with HER2 mutations: a multicenter, single-arm, phase II trial. BMC Medicine. 2022 Feb 01;20(1):42. doi: 10.1186/s12916-022-02245-z.
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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