= 926927-61-9 [标题:Reaction Conditions 标题:8-Substituted Benzoazepines As Toll-Like Receptor Modulators 参考文献:United States
(Tert-Butoxy)-N-{4-(N,N-Dipropylcarbamoyl)-8-[4-(Pyrrolidinylcarbonyl)Phenyl](3H-Benzo[f]Azepin-2-yl)}Carboxamide置于三氟乙酸,碳酸氢钠体系中,用 二氯甲烷,水 作为反应溶剂,以92.3%的收率获得产物motolimod(莫托莫德) 参考文献: Methods Of Synthesis Of Benzazepine Derivatives[fr] Procédés De Synthèse De Dérivés De Benzazépine 标题: Methods Of Synthesis Of Benzazepine Derivatives[fr] Procédés De Synthèse De Dérivés De Benzazépine 摘要:该披露描述了合成取代苯并哌啶衍生物的方法.根据该披露的首选方法,允许大规模制备低金属杂质水平的苯并哌啶化合物.在某些实施例中,根据该披露的首选方法还可以在比先前用于制备这类化合物的方法更高的产率下制备苯并哌啶衍生物,而无需使用色谱纯化方法.本披露的方法在合成有机化学和药物化学中具有实用性.
专利号:US-8314090-B2 优先权日:2008-11-06 标 题:Methods of synthesis of benzazepine derivatives 发明人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON 权利人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON; VENTIRX PHARMACEUTICALS INC; ARRAY BIOPHARMA INC 摘要:The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-2022259212-A1 优先权日:2019-07-11 标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase 发明人:BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.
专利号:ES-2705101-T3 优先权日:2008-11-06 标 题:Methods of synthesis of benzazepine derivatives
专利号:CA-2742863-C 优先权日:2008-11-06 标题 :Methods of synthesis of benzazepine derivatives
专利号:AU-2009313392-B2 优先权日:2008-11-06 标题 :Methods of synthesis of benzazepine derivatives
1: Yang W, Sun X, Liu S, Xu Y, Li Y, Huang X, Liu K, Mao L, Min S, Liu L, Li S, Zhu Y, Zhang Y, Xie X, Xu K, Sun C, Yan J, Li Z. TLR8 agonist Motolimod-induced inflammatory death for treatment of acute myeloid leukemia. Biomed Pharmacother. 2023 Jul;163:114759. doi: 10.1016/j.biopha.2023.114759. Epub 2023 Apr 25. 179:112987. doi: 10.1016/j.jpba.2019.112987. Epub 2019 Nov 12. 167:90-99. doi: 10.1016/j.jpba.2019.02.009. Epub 2019 Feb 7. 4(11):1583-1588. doi: 10.1001/jamaoncol.2018.1888.
合成参考文献
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