CAS: 203258-60-0; 4-(2-Bromoacrylamido)-N-(5-((5-((5-((2-Guanidinoethyl)Carbamoyl)-1-Methyl-1H-Pyrrol-3-yl)Carbamoyl)-1-Methyl-1H-Pyrrol-3-yl)Carbamoyl)-1-Methyl-1H-Pyrrol-3-yl)-1-Methyl-1H-Pyrrole-2-Carboxamide

结构式图片

MSDS等安全信息

    合成工艺路线路线简述

      📜4-[(2-Bromoacryloyl)Amino]-1-Methyl-1H-Pyrrole-2-Carboxylic Acid Chloride,4-Amino-N-[5-[[5-[2-(Diaminomethylideneamino)Ethylcarbamoyl]-1-Methylpyrrol-3-Yl]Carbamoyl]-1-Methylpyrrol-3-Yl]-1-Methylpyrrole-2-Carboxamide 反应生成 N-(5-{[(5-{[(5-{[(2-{[Amino(Imino)Methyl]Amino}Ethyl) Amino]Carbonyl}-1-Methyl-1H-Pyrrol-3-yl)Amino]Carbonyl}-1-Methyl-1H-Pyrrol-3-yl)Amino]Carbonyl}-1-Methyl-1H-Pyrrol-3-yl)-4-[(2-Bromoacryloyl)Amino]-1-Methyl-1H-Pyrrole-2-Carboxamide
      参考文献:Cytotoxic α-Bromoacrylic Derivatives Of Distamycin Analogues Modified At The Amidino Moiety
      标题:Cytotoxic α-Bromoacrylic Derivatives Of Distamycin Analogues Modified At The Amidino Moiety
      摘要:The Design,Synthesis,In Vitro And In Vivo Activities Of Novel Alpha-Bromoacrylic Derivatives Of Distamycin A,Modified At The Amidino Moiety By The Replacement With Basic Or Non-Basic Groups Are Reported. In Spite Of The Relevance Of These Modifications Of Distamycin Frame,The New Derivatives Are Potent Cytotoxics. The Presence Of The Amidino Moiety,Is,Therefore,Not An Absolute Requirement For The Activity. In Particular Due To A Favorable Myclotoxicity/Cytotoxicity Ratio,Guanidino Derivative Pnu 166196 Was Selected For Clinical Development. (C) 2000 Elsevier Science Ltd. All Rights Reserved.
      Doi:10.1016/S0960-894X(00)00205-5

      海关参考信息

      专利信息


      专利号:US-12391691-B2
      优先权日:2018-11-16
      标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
      发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
      权利人:AMGEN INC
      摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

      专利号:US-2025206736-A1
      优先权日:2019-11-14
      标题 :Synthesis of kras g12c inhibitor compound
      发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
      权利人:AMGEN INC
      摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

      专利号:US-2017283878-A1
      优先权日:2015-12-11
      标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
      发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
      权利人:ACADEMIA SINICA
      摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

      专利号:US-2023192681-A1
      优先权日:2019-11-14
      标 题 :Improved synthesis of kras g12c inhibitor compound

      专利号:US-10272065-B2
      优先权日:2013-01-14
      标题 :Gem-difluorinated C-glycoside compounds as anti-cancer agents
      发明人:SLILATY STEVE N
      权利人:ADVANOMICS CORP; BENOIT & COTE
      摘要:The present document describes a synthesis of a class of gem-difluorinated C-glycoside compounds derived from podophyllotoxin, which may be used, but not exclusively, in oncology for the treatment of cancer. More particularly, the podophyllotoxin gem-difluorinated C-glycoconjugated derivatives display improved conformational and chemical stability, and improved cytotoxicity exhibited against drug-resistant cancer cell lines.

      专利号:US-11299491-B2
      优先权日:2018-11-16
      标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound

      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. Caponigro, F.; Lorusso, D.; Fornari, G.; Barone, C.; Merlano, M.; Airoldi, M.; Schena, M.; MacArthur, R.; Weitman, S.; Jannuzzo, M. G.; Crippa, S.; Fiorentini, F.; Petroccione, A.; Comis, S. Phase I dose-escalation study of brostallicin, a minor groove binder, in combination with cisplatin in patients with advanced solid tumors. Cancer Chemotherapy and Pharmacology (2010), 66(2), 389-394. CODEN: CCPHDZ ISSN:0344-5704. AN
      2010:622626 2. Pezzola, Silvia; Antonini, Giovanni; Geroni, Cristina; Beria, Italo; Colombo, Maristella; Broggini, Massimo; Marchini, Sergio; Mongelli, Nicola; Leboffe, Loris; MacArthur, Robert; Mozzi, Alessia Francesca; Federici, Giorgio; Caccuri, Anna Maria. Correction to Role of Glutathione Transferases in the Mechanism of Brostallicin Activation. Biochemistry (2010), 49(23), 4930. CODEN: BICHAW ISSN:0006-2960. AN
      2010:618736 3. Rickles, Richard; Lee, Margaret S.  -Adrenergic receptor agonists for the treatment of B-cell proliferative disorders. PCT Int. Appl. (2009), 111 pp. CODEN: PIXXD2 WO 2009151569 A2 20091217 CAN
      152:67621 AN

      合成参考文献


      摘要:Geroni C, Marchini S, Cozzi P, Galliera E, Ragg E, Colombo T, Battaglia R, Howard M, D'Incalci M, Broggini M. Brostallicin, a novel anticancer agent whose activity is enhanced upon binding to glutathione. Cancer Res. 2002 Apr 15;62(8):2332–6.
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