CAS: 1130115-44-4; 4-(4-(3-(4-Chloro-3-(Trifluoromethyl)Phenyl)Ureido)Phenoxy)-N-(Methyl-D3)Picolinamide

该化合物是索拉芬尼布(Sorafenib)的绝缘类比,一种众所周知的多因子酶抑制剂.在特定位置用除子原子代替氢来代替氢能,可以提高化合物代谢稳定性,从而有可能改善其药用动力学特征.这一修改可以导致氧化新陈代谢的减少,延长半衰期,并比非脱氧形式增加生物利用率.Sorafenib-d主要用作生物基质中精确测量索拉芬尼布的定量质谱测量的内部标准.其结构相似性确保可靠的分析性,而其同位素标签可以进行不同的检测.这一化合物对于涉及索拉芬尼布的代谢,分布和药用对地基分析的研究和临床研究很有价值.

结构式图片

物理性质

MSDS等安全信息

    上下游产品

    索拉非尼相关化合物a 4-(4-(3-(4-Chloro-3-(Trifluoromethyl)Phenyl)Ureido)Phenoxy)Picolinic Acid 1012058-78-4
    4-(4-(3-(4-氯-3-(三氟甲基)苯基)脲啶)苯氧基)吡啶甲酸甲酯 Methyl 4-(4-(3-(4-Chloro-3-(Trifluoromethyl)Phenyl)Ureido)Phenoxy)Picolinate 573673-43-5
    索拉非尼叔丁酯 Tert-Butyl 4-(4-(3-(4-Chloro-3-(Trifluoromethyl)Phenyl)Ureido)Phenoxy)Picolinate 1097726-89-0
    [4-(4-氨基苯氧基)(2-吡啶基)]-N-(甲基-D3)甲酰胺 4-(4-Aminophenoxy)-N-(Methyl-D3)Picolinamide 1189975-18-5
    1-(4-Chloro-3-(Trifluoromethyl)Phenyl)-3-(4-Methoxyphenyl)Urea 893004-65-4
    1-(4-氯-3-(三氟甲基)苯基)-3-(4-羟基苯基)脲 1-(4-Chloro-3-(Trifluoromethyl)Phenyl)-3-(4-Hydroxyphenyl)Urea 1129683-83-5

    合成工艺路线路线简述

      📜4-(4-氨基苯氧基)吡啶甲酸叔丁酯置于三乙基硅烷,N,N-二异丙基乙胺,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-),三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 48.0H,反应生成索拉非尼-D3
      参考文献:Method And Process For Preparation And Production Of Deuterated Omega-Diphenylurea
      标题:Method And Process For Preparation And Production Of Deuterated Omega-Diphenylurea
      摘要:揭示了制备和生产重氮化ω-二苯脲的方法和过程.特别是,揭示了一种可以抑制磷酸激酶的重氮化ω-二苯脲化合物以及n-(4-氯-3-(三氟甲基)苯基-N'-(4-(2-(N-D3-甲基氨基甲酰)-4-吡啶氧基)苯基)尿素的制备方法.所述的重氮化二苯脲化合物可用于治疗或预防肿瘤及相关疾病.

      海关参考信息

      专利信息


      专利号:WO-2023227996-A1
      优先权日:2022-05-24
      标题 :A deuterated amine compounds and process for synthesis thereof
      发明人：AMBATI VIJAY; KOTHARI MANISH; JONNALAGADDA NAGASIVARAO; ALETI RANJITH; KANDASAMY DR SAKHTIVEL; ROHIT CHITTALURI KRISHNA; REDDY KATUKURI MALLIKHARJUNA
      权利人:CLEARSYNTH LABS LTD
      摘要:The present invention relates to a process for synthesis of a deuterated compound. Most particularly, it relates to synthesis of a deuterated amine compounds of formula (l) and salts thereof. The said compound is an important key intermediate in the synthesis of deuterated drugs and/or chemical compounds.

      专利号:CN-118454599-A
      优先权日:2024-04-29
      标题:Continuous flow synthesis method of deuterated dimethylamine hydrochloride

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      主要参考文献


      1: Ho V, Lim TS, Lee J, Steinberg J, Szmyd R, Tham M, Yaligar J, Kaldis P, Abastado JP, Chew V. TLR3 agonist and Sorafenib combinatorial therapy promotes immune activation and controls hepatocellular carcinoma progression. Oncotarget. 2015 Jul 23. [Epub ahead of print] doi: 10.1159/000343861. Review.
      3: Kudo M. Biomarkers and Personalized Sorafenib Therapy. Liver Cancer. 2014 Oct;3(3-4):399-404. doi: 10.1159/000343870.
      4: Erika G, Federica Z, Martina S, Anselmo P, Luigi R, Marina M, Davide C, Eleonora Z, Monica V, Silverio T. Old tyrosine kinase inhibitors and newcomers in gastrointestinal cancer treatment. Curr Cancer Drug Targets. 2015 Aug 17. [Epub ahead of print] doi: 10.1371/journal.pone.0134731. eCollection 2015. doi: 10.4254/wjh.v7.i16.2029. Review.

      合成参考文献


      摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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