CAS: 146943-43-3; (S)-Diethyl 2-(4-(2-(2-Amino-4-Oxo-4,7-Dihydro-3H-Pyrrolo[2,3-D]Pyrimidin-5-yl)Ethyl)Benzamido)Pentanedioate

该化合物是一个复杂的有机化合物,具有多功能结构特征.该化合物具有一个以其生物活动,特别是药用化学活动而闻名的闪光性核心.二乙基酯组的存在表明它具有溶解有机溶剂溶解性的潜力,适合各种化学反应和应用.该化合物还含有一个氨基化合物,有助于其反应和与生物目标的潜在互动.该化合物的苯并表明它可能与芳香系统发生相互作用,加强其药理特性.

结构式图片

MSDS等安全信息

    上下游产品

    CAS号1118-89-4 L-谷氨酸二乙酯盐酸盐 | CAS号137281-39-1 培美酸 | CAS号243636-78-4 diethyl N-{4-[2... | CAS号3140-73-6 2-氯-4,6-二甲氧基-1,... | CAS号348620-55-3 2-amino-4-oxo-5... | CAS号348620-17-7 methyl N-crotyl... | CAS号65874-27-3 4-甲酰基苯甲酸叔丁酯 | CAS号146943-27-3 methyl 3-[4-(te... | CAS号243636-63-7 methyl N-crotyl... | CAS号151864-81-2 对乙氧基甲酰苯丙醛 | CAS号165049-28-5 N-(4-[2-(2-氨基-4...

    合成工艺路线路线简述

      4-(3-甲酰基丙基)苯甲酸乙酯置于n-甲基吗啉,盐酸,2-氯-4,6-二甲氧基-1,3,5-三嗪,5,5-二溴-2,2-二甲基-4,6-二酮-1,3-二氧杂环己烷,Sodium Acetate,Sodium Hydroxide体系中,用 甲醇,乙醚,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 57.0H,反应生成N-(4-(2-(2-氨基-4-氧代-4,7-二氢-3H-吡咯并[2,3-D]嘧啶-5-基)乙基)苯甲酰基)-L-谷氨酸二乙酯
      参考文献:Discovery Of 5-Substituted Pyrrolo[2,3-D]Pyrimidine Antifolates As Dual-Acting Inhibitors Of Glycinamide Ribonucleotide Formyltransferase And 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase In De Novo Purine Nucleotide Biosynthesis: Implications Of Inhibiting 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase To Ampk Activation And Antitumor Activity
      标题:Discovery Of 5-Substituted Pyrrolo[2,3-D]Pyrimidine Antifolates As Dual-Acting Inhibitors Of Glycinamide Ribonucleotide Formyltransferase And 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase In De Novo Purine Nucleotide Biosynthesis: Implications Of Inhibiting 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase To Ampk Activation And Antitumor Activity
      摘要:We Synthesized 5-Substituted Pyrrolo[2,3-D]Pyrimidine Antifolates (Compounds 5-10) With One-To-Six Bridge Carbons And A Benozyl Ring In The Side Chain As Antitumor Agents. Compound 8 With A 4-Carbon Bridge Was The Most Active Analogue And Potently Inhibited Proliferation Of Folate Receptor (Fr) Alpha-Expressing Chinese Hamster Ovary And Kb Human Tumor Cells. Growth Inhibition Was Reversed Completely Or In Part By Excess Folic Acid,Indicating That Fr Alpha Is Involved In Cellular Uptake,And Resulted In S-Phase Accumulation And Apoptosis. Antiproliferative Effects Of Compound 8 Toward Kb Cells Were Protected By Excess Adenosine But Not Thymidine,Establishing De Novo Purine Nucleotide Biosynthesis As The Targeted Pathway. However,5-Aminoimidazole-4-Carboxamide (Aica) Protection Was Incomplete,Suggesting Inhibition Of Both Aica Ribonucleotide Formyltransferase (Aicarftase) And Glycinamide Ribonucleotide Formyltransferase (Garftase). Inhibition Of Garftase And Aicarftase By Compound 8 Was Confirmed By Cellular Metabolic Assays And Resulted In Atp Pool Depletion. To Our Knowledge,This Is The First Example Of An Antifolate That Acts As A Dual Inhibitor Of Garftase And Aicarftase As Its Principal Mechanism Of Action.
      Doi:10.1021/jm401328U

      海关参考信息

      专利信息


      专利号:US-8981090-B2
      优先权日:2010-07-22
      标 题:Process for the synthesis of pemetrexed disodium salt
      发明人:CIAMBECCHINI UMBERTO; TURCHETTA STEFANO; ZENONI MAURIZIO; DE FERRA LORENZO; BRANDI PAOLO
      权利人:CIAMBECCHINI UMBERTO; TURCHETTA STEFANO; ZENONI MAURIZIO; DE FERRA LORENZO; BRANDI PAOLO; CHEMI SPA
      摘要:The present invention relates to a novel process for the preparation of pemetrexed diethyl ester 2 n nby purifying the mixture obtainable by reacting compounds 1 and 1a in the presence of a chemical agent capable of promoting the formation of a peptide bond in an aprotic organic solventn n ncharacterized in that the mixture is subjected to the following steps:n a) washing with a basic aqueous solution; b) concentration of the organic phase; c) addition of a polar organic solvent and/or a mixture of polar organic solvents; d) precipitation of the pemetrexed diethyl ester 2.

      专利号:EP-2409978-A2
      优先权日:2010-07-22
      标 题 :A novel process for the synthesis of pemetrexed disodium salt

      专利号:TW-201209058-A
      优先权日:2010-07-22
      标 题 :A novel process for the synthesis of pemetrexed disodium salt

      专利号:US-2012172595-A1
      优先权日:2010-07-22
      标题:Novel process for the synthesis of pemetrexed disodium salt

      专利号:CN-102344452-A
      优先权日:2010-07-22
      标 题 :A new method for the synthesis of pemetrexed disodium salt

      专利号:EP-2409978-B1
      优先权日:2010-07-22
      标 题 :A novel process for the synthesis of pemetrexed disodium salt
      武汉康蓝药业有限公司
      ⚠️ 未注册 · 未认证企业
      ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
      数据来源于公开网络搜索,平台未作核实,请自行辨别。
      🏢敬请 企业认领
      🏬开设公司展台
      📢获取免费会员权益
      🎖️点亮专属注册企业标签
      📇展现公司完整信息 样本查看立即注册认领 →
      网址: http://www.calmlandpharma.com
      电话: 027-59884202👤
      📞武汉康蓝药业有限公司 ⚠️参考联系方式

      销售电话:027-59884202
      邮箱:ryan@aiconland.com
      🆔 联系时候可告知是从"百琢研"平台获取的信息.
      ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

      ⚠️ 未注册 · 未认证企业
      注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别 ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
      第 1 / 1 页
      现货

      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. Ramalingam SS, Dahlberg SE, Belani CP, Saltzman JN, Pennell NA, Nambudiri GS, McCann JC, Winegarden JD, Kassem MA, Mohamed MK, Rothman JM, Lyss AP, Horn L, Stinchcombe TE, Schiller JH. Pemetrexed, Bevacizumab, or the Combination As Maintenance Therapy for Advanced Nonsquamous Non-Small-Cell Lung Cancer: ECOG-ACRIN 5508. J Clin Oncol. 2019 Sep 10;37(26):2360-2367. doi: 10.1200/JCO.19.01006. Epub 2019 Jul 30.
      2: Vora, P. A., Patel, R., & Dharamsi, A. (2021). Pemetrexed–first-line therapy for non-squamous non-small cell lung cancer: a review of patent literature. Recent Patents on Anti-Cancer Drug Discovery, 16(3), 333-349.

      合成参考文献


      参考文献:10.1055/s-0037-1610320
      摘要:Menéndez J, Leonardi M, Estévez V, Villacampa M. The Hantzsch Pyrrole Synthesis: Non-conventional Variations and Applications of a Neglected Classical Reaction. Synthesis. 2018 Dec 03;51(04):816–28. doi: 10.1055/s-0037-1610320.
      📝 需求与反馈
      尽可能描述清楚需求与问题信息
      ×

      通知