CAS: 1056634-68-4; N-(Cyanomethyl)-4-(2-((4-Morpholinophenyl)Amino)Pyrimidin-4-yl)Benzamide

该化合物是一种针对Janus kinase 1和JAK2的小型分子抑制剂,以及A受体1型的活性物质(ACVR1).主要针对治疗宫颈膜纤维化(一种新生肿瘤)的情况进行调查.Momenotinib的双重行动机制不仅抑制了JAK-STAT的信号信号,减少了炎症和症状负担,而且还通过ACVR1抑制剂调节肝炎生产,解决了贫血--一种常见的宫颈膜炎病人的共性.它能够改善血清,立体症状和贫血症状,并将其与其他日本乳房癌抑制剂区别开来.复合物展示了可喜的药用植物动力学,并在第三阶段试验中展示了临床功效,使它成为中度或高风险小叶霉素患者有希望的治疗选择.

结构式图片

欧盟法规

REACH注册C&L通报

上下游产品

4-(2-(4-吗啉苯基氨基)嘧啶-4-基)苯甲酸 4-{2-[(4-Morpholinophenyl)Amino]Pyrimidin-4-Yl}Benzoic Acid 945749-71-3
Methyl 4-(2-((4-Morpholinophenyl)Amino)Pyrimidin-4-yl)Benzoate
4-(2-(4-吗啉苯基氨基)嘧啶-4-基)苯甲酸乙酯 Ethyl 4-(2-((4-Morpholinophenyl)Amino)Pyrimidin-4-yl)Benzoate 1056634-62-8

合成工艺路线路线简述

  • 合成目标产物 Momelotinib 主要起始原料 4-(2-(4-Morpholinophenylamino)Pyrimidin-4-yl)Benzoic Acid And Aminoacetonitrile Hydrochloride
  • (文献来源)合成步骤主要原料 4-(2-(4-Morpholinophenylamino)Pyrimidin-4-yl)Benzoic Acid 和 Aminoacetonitrile Hydrochloride
4-乙酰基苯甲酸甲酯置于水,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺,Sodium Hydroxide体系中,用 甲醇,N,N-二甲基甲酰胺,甲苯,乙腈 用作溶剂,化学反应 28.0H,反应生成莫洛替尼
参考文献:通过钯催化的芳族羧酸与官能化脂肪腈的脱羧加成/环化反应序列合成咪唑和恶唑
标题:通过钯催化的芳族羧酸与官能化脂肪腈的脱羧加成/环化反应序列合成咪唑和恶唑
摘要:我们在此报告了一种以单步方式组装多取代咪唑和恶唑的有效方法.这些转化基于容易获得的芳香族羧酸和脂肪族腈的脱羧加成和环化,并表现出非常好的官能团兼容性和高步骤经济性.该反应是可扩展的,制备的产品可以转化为实用的骨架.重要的是,莫罗替尼的后期衍生化突出了这种方法的潜在效用.
Doi:10.1021/acs.Orglett.1C01762

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-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

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:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound
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主要参考文献


1: Palandri F, Schaap NPM, Rey J, von Bubnoff N, Reiter A, Hernandez-Boluda JC, Devos T, Nilsson L, Psaila B, McLornan DP, Strouse B, Zhang S, Patel B, Lim J, Patnaik D, Oh ST. Spleen Volume Reduction and Transfusion Independence With Momelotinib Versus Ruxolitinib and Associated Overall Survival With Momelotinib in JAK Inhibitor-Naive Patients With Myelofibrosis and Anemia: Subgroup Analyses of SIMPLIFY-1. Clin Lymphoma Myeloma Leuk. 2026 Feb
14:S2152-2650(26)00039-X. doi: 10.1016/j.clml.2026.02.004. Epub ahead of print. 105(4):133. doi: 10.1007/s00277-026-06873-w.
3: Zhang Y, Zhang H, Hu N, Yang L, Liu Y, Yang L, Dong X, Wang H. The Immunoregulatory and Hematopoietic Effects of Momelotinib in a Murine Bone Marrow Failure Model. J Clin Lab Anal. 2026 Feb;40(4):e70161. doi: 10.1002/jcla.70161. Epub 2026 Jan 19.

合成参考文献


摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
参考文献:10.1177/2168479017750129
摘要:Baldrick P. Juvenile Animal Testing: Assessing Need and Use in the Drug Product Label. Ther Innov Regul Sci. 2018 Sep;52(5):641–8. doi: 10.1177/2168479017750129.
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