CAS: 1073154-85-4; N-Methyl-4-((4-(((3-(N-Methylmethylsulfonamido)Pyrazin-2-yl)Methyl)Amino)-5-(Trifluoromethyl)Pyrimidin-2-yl)Amino)Benzamide

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上下游产品

4-((4-chloro-5-(trifluoromethyl)pyrimidin-2-yl)amino)-N-methylbenzamide 4-amino-N-methyl-benzamide

合成工艺路线路线简述

    📜Tert-Butyl 4-((4-Chloro-5-(Trifluoromethyl)Pyrimidin-2-yl)Amino)Benzoate置于盐酸,N,N-二异丙基乙胺,N,N'-羰基二咪唑体系中,用 1,4-二氧六环,N-甲基吡咯烷酮,二氯甲烷 用作溶剂,化学反应 14.0H,反应生成地法替尼
    参考文献: Synthesis Method For Aminopyrimidine Fak Inhibitor Compound[fr] Procédé De Synthèse D'Un Composé Inhibiteur D'Aminopyrimidine Fak[zh] 一种合成氨基嘧啶类fak抑制剂化合物的方法
    标题: Synthesis Method For Aminopyrimidine Fak Inhibitor Compound[fr] Procédé De Synthèse D'Un Composé Inhibiteur D'Aminopyrimidine Fak[zh] 一种合成氨基嘧啶类fak抑制剂化合物的方法
    摘要:一种合成氨基嘧啶类fak抑制剂化合物的方法,涉及药物合成领域.合成方法包括如下步骤:其中,R1为氢或羧酸保护基,R2选自c1~c6烷基或c1~c6氘代烷基,R3和r4分别独立选自氢或氘,R5选自c1~c6烷基或c1~c6氘代烷基.合成方法操作简便,成本低;制备得到的产品却能够获得很高的总收率(>=66%)和纯度(>=99%),产品收率和纯度优于现有技术(现有技术总收率为11%左右,纯度为99%).合成方法取得了优异的效果,还可成功地制备公斤级终产物,适于工艺生产,具有非常好的应用前景.

    专利信息


    专利号:US-2024059678-A1
    优先权日:2021-01-18
    标 题 :Synthesis Method for Aminopyrimidine FAK Inhibitor Compound
    发明人:DU WU; LV HAIBIN; LI YU; KUANG TONGTAO; GENG XI
    权利人:HINOVA PHARMACEUTICALS INC
    摘要:A synthesis method for an aminopyrimidine FAK inhibitor compound, relating to the field of pharmaceutical synthesis. In the synthesis method, R1 is hydrogen or a carboxylic acid protecting group, R2 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl, R3 and R4 are each independently selected from hydrogen or deuterium, and R5 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl. The synthesis method is simple to operate, and has low costs. The product prepared can obtain a high total yield (≥66%) and a high purity (≥99%), and the product yield and purity are superior to those in the prior art (in the prior art, the total yield is about 11%, and the purity is 99%). The synthesis method achieves excellent effects, can also successfully prepare a final product on kilogram scale, and is suitable for industrial production, having a good application prospect.

    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.

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    📌 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: Ryzhakov G, Almuttaqi H, Corbin AL, Berthold DL, Khoyratty T, Eames HL, Bullers S, Pearson C, Ai Z, Zec K, Bonham S, Fischer R, Jostins-Dean L, Travis SPL, Kessler BM, Udalova IA. Defactinib inhibits PYK2 phosphorylation of IRF5 and reduces intestinal inflammation. Nat Commun. 2021 Nov 18;12(1):6702. doi: 10.1038/s41467-021-27038-5.
    2: Wang-Gillam A, Lim KH, McWilliams R, Suresh R, Lockhart AC, Brown A, Breden M, Belle JI, Herndon J, Bogner SJ, Pedersen K, Tan B, Boice N, Acharya A, Abdiannia M, Gao F, Yoon HH, Zhu M, Trikalinos NA, Ratner L, Aranha O, Hawkins WG, Herzog BH, DeNardo DG. Defactinib, Pembrolizumab, and Gemcitabine in Patients with Advanced Treatment Refractory Pancreatic Cancer: A Phase I Dose Escalation and Expansion Study. Clin Cancer Res. 2022 Dec 15;28(24):5254-5262. doi: 10.1158/1078-0432.CCR-22-0308.
    3: Hosein AN, Brekken RA, Maitra A. Pancreatic cancer stroma: an update on therapeutic targeting strategies. Nat Rev Gastroenterol Hepatol. 2020 Aug;17(8):487-505. doi: 10.1038/s41575-020-0300-1. Epub 2020 May 11.

    合成参考文献


    摘要:
    摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).
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