CAS: 1132935-63-7; N-(6-(3-(Tert-Butyl)-5-(2,4-Dioxo-3,4-Dihydropyrimidin-1(2H)-yl)-2-Methoxyphenyl)Naphthalen-2-yl)Methanesulfonamide

上下游产品

1-(3-Tert-Butyl-5-(6-Hydroxynaphthalen-2-yl)-4-Methoxyphenyl)-Pyrimidine-2,4(1H,3H)-Dione 1355646-93-3
6-(3-Tert-Butyl-5-(2,4-Dioxo-3,4-Dihydropyrimidin-1(2H)-yl)-2-Methoxyphenyl)Naphthalen-2-Yl 1,1,2,2,3,3,4,4,4-Nonafluorobutane-1-Sulfonate 1355646-97-7
1-(3-叔丁基-5-碘-4-甲氧基苯基)嘧啶-2,4(1H,3H)-二酮 1-(3-Tert-Butyl-5-Iodo-4-Methoxyphenyl)-2,4-Dihydropyrimidine-2,4(1H,3H)-Dione 1132940-53-4
1-(3-Bromo-5-Tert-Butyl-4-Methoxyphenyl)Pyrimidine-2,4(1H,3H)-Dione 1132942-12-1

2-叔丁基苯酚置于potassium Phosphate,Tris-(Dibenzylideneacetone)Dipalladium(0),Copper(L) Iodide,2-(2-吡啶)-苯并咪唑,2-二叔丁基膦-2',4',6'-三异丙基-3,6-二甲氧基-1,1'-联苯,Potassium Carbonate,Sodium Hydroxide,1,3,5,7-四甲基-6-苯基-2,4,8-三氧杂-6-磷酰金刚烷体系中,用 四氢呋喃,2-甲基四氢呋喃,甲醇,水,二甲基亚砜,乙酸乙酯,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 40.5H,反应生成达沙布韦
参考文献:金属催化偶联反应在合成 Hcv 聚合酶抑制剂 Dasabuvir 中的发现和发展.
标题:金属催化偶联反应在合成 Hcv 聚合酶抑制剂 Dasabuvir 中的发现和发展.
摘要:Dasabuvir ( 1 ) 是一种 Hcv 聚合酶抑制剂,已被开发为三组分直接作用抗病毒联合疗法的一部分.在合成路线的开发过程中,开发了两种新的偶联反应.首先,发现了使用吡啶酰胺16作为配体的尿嘧啶与芳基碘化物的铜催化偶联.后来,在富电子钯配合物(包括新型膦配体 Vincephos ( 50 ))的推动下,开发了钯催化的芳基非磺酸盐33 的磺酰胺化反应.这使得达沙布韦的收敛,高效合成成为可能,显着降低了该过程的诱变杂质负担.
Doi:10.1021/acs.Joc.8B02690

专利信息

专利号:US-2024207302-A1
优先权日:2021-04-01
标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof
发明人：CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.

专利号:US-12404246-B1
优先权日:2024-10-01
标 题:2-aminomethylimidazole mimics of NS4A and their effect thereof on hepatitis C virus NS3 protease
发明人：BARADWAN MOHAMMED A; OMAR ABDELSATTAR M; ELFAKY MAHMOUD A; EL-ARABY MOUSTAFA E; SOROR SAMEH H
权利人:BARADWAN MOHAMMED A; OMAR ABDELSATTAR M; ELFAKY MAHMOUD A; EL ARABY MOUSTAFA E; SOROR SAMEH H; UNIV KING ABDULAZIZ
摘要:Chronic hepatitis C is a global health problem affecting large number of people and leads to mortalities and morbidities. In this invention, new compounds belonging to 2-substituted-1H-imidazole-4-carboxamide derivatives (Formula I) intended for use in the treatment of hepatitis C are disclosed. The compounds interfere with the important viral peptide NS4A co-enzyme function. The described art includes chemical synthesis, spectral confirmation and binding assays with NS3 protein.

专利号:US-2022411407-A1
优先权日:2019-11-15
标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
发明人：WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

专利号:US-2021290651-A1
优先权日:2020-03-20
标 题:Methods of treating viral infections using inhibitors of nucleotide synthesis pathways

专利号:US-2021308117-A1
优先权日:2020-03-20
标 题 :Methods of treating viral infections using inhibitors of nucleotide synthesis pathways

专利号:US-2021315880-A1
优先权日:2020-03-20
标 题 :Methods of treating viral infections using inhibitors of nucleotide synthesis pathways