CAS: 1338225-97-0; 3-Chloro-5-((1-((4-Methyl-5-Oxo-4,5-Dihydro-1H-1,2,4-Triazol-3-yl)Methyl)-2-Oxo-4-(Trifluoromethyl)-1,2-Dihydropyridin-3-yl)Oxy)Benzonitrile

上下游产品

3-Chloro-5-((2-Oxo-1-((5-Oxo-4,5-Dihydro-1H-1,2,4-Triazol-3-yl)Methyl)-4-(Trifluoromethyl)-1,2-Dihydropyridin-3-yl)Oxy)Benzonitrile 1338226-05-3
3-Chloro-5-((1-((1-(2-Methoxypropan-2-yl)-4-Methyl-5-Oxo-4,5-Dihydro-1H-1,2,4-Triazol-3-yl)Methyl)-2-Oxo-4-(Trifluoromethyl)-1,2-Dihydropyridin-3-yl)Oxy)Benzonitrile 1613307-25-7
3-氯-5-[[2-氧代-4-(三氟甲基)-1,2-二氢吡啶-3-基]氧基]苯甲腈 3-Chloro-5-((2-Oxo-4-(Trifluoromethyl)-1,2-Dihydropyridin-3-yl)Oxy)Benzonitrile 1155846-86-8
3-(3-Bromo-5-Chlorooxy)-4-(Trifluoromethyl)Pyridin-2(1H)-One 1155846-88-0

📜3-Chloro-5-((1-((1-(2-Methoxypropan-2-yl)-4-Methyl-5-Oxo-4,5-Dihydro-1H-1,2,4-Triazol-3-yl)Methyl)-2-Oxo-4-(Trifluoromethyl)-1,2-Dihydropyridin-3-yl)Oxy)Benzonitrile 以46的收率获得多拉韦林
参考文献: Process For Making Reverse Transcriptase Inhibitors[fr] Procédé De Préparation D'Inhibiteurs De Transcriptase Inverse
标题: Process For Making Reverse Transcriptase Inhibitors[fr] Procédé De Préparation D'Inhibiteurs De Transcriptase Inverse
摘要:本发明涉及一种合成3-(取代苯氧基)-1-[(5-氧代-4,5-二氢-1H-1,2,4-三唑-3-基)甲基]-吡啶-2(1H)-酮衍生物的新工艺.本发明的合成方法所得到的化合物是hiv反转录酶抑制剂,可用于抑制反转录酶,Hiv复制以及治疗人体免疫缺陷病毒感染.

专利信息

专利号:US-2025179033-A1
优先权日:2021-12-30
标 题 :New antiviral triazole derivatives, their synthesis and their use for treatment of mammalian viral infections
发明人：MAKAROV VADIM; RIABOVA OLGA; LANE THOMAS R; EKINS SEAN
权利人:COLLABORATIONS PHARMACEUTICALS INC; FEDERAL RES CENTER FUNDAMENTALS OF BIOTECHNOLOGY RUSSIAN ACADEMY OF SCIENCE
摘要:A family of triazole derivatives is described. Also described is the use of these triazole derivatives in treating or preventing viral infections, such as human immunodeficiency virus (HIV) infections, and the diseases caused by these infections, such as acquired immunodeficiency syndrome (AIDS). The triazole derivatives, for example, comprise a central triazole group with two substituents comprising an aryl or heteroaryl group. Exemplary derivatives showed excellent HIV inhibitory activity against both wild-type and selected mutant strains of HIV.

专利号:WO-2025124470-A1
优先权日:2023-12-15
标 题:Doravirine intermediate, and use thereof and synthesis method therefor
发明人：GAO ZHANGBIN; WEN SHAOPENG; YANG JINHONG; JU JINGJING; MAO WENXIU
权利人:SHANDONG CHENGCHUANG BLUE SEA PHARMACEUTICAL TECH CO LTD
摘要:The present invention relates to a doravirine intermediate, and the use thereof and a synthesis method therefor, which belong to the technical field of pharmaceutical chemistry. The method for synthesizing the doravirine intermediate comprises the following steps: (1) mixing ethyl 2-fluoroacetate with 4-ethoxy-1,1,1-trifluoro-3-buten-2-one with solvent I, and then dropwise adding sodium bis(trimethylsilyl)amide to form compound 1; (2) adding an ammonia source into the reaction liquid of compound 1 to obtain compound 2; (3) dissolving compound 2 in solvent II, adding a catalyst, and heating and ring-closing the mixture to obtain compound 3; and (4) dissolving compound 3 in toluene, adding thionyl chloride, and dropwise adding pyridine to obtain 2-hydroxy-3-fluoro-4-trifluoromethylpyridine. The synthesis method of the present invention has a low raw material cost and a short process period, is environmentally friendly, and is suitable for process scaled-up production.

专利号:WO-2025124469-A1
优先权日:2023-12-15
标 题 :Method for synthesizing doravirine intermediate
发明人：GAO ZHANGBIN; XU FANGHUI; ZHAO XINYU; JU JINGJING; MAO WENXIU
权利人:SHANDONG CHENGCHUANG BLUE SEA PHARMACEUTICAL TECH CO LTD
摘要:The present invention relates to the technical field of pharmaceutical chemistry, and to a method for synthesizing a doravirine intermediate. The synthesis method of the present invention comprises: (1) mixing ethyl 2-fluoroacetate with 4-ethoxy-1,1,1-trifluoro-3-buten-2-one in a first solvent and adding sodium bis(trimethylsilyl)amide for a reaction to generate compound 1; (2) adding triethylamine and trifluoroacetic anhydride to a reaction solution of compound 1 for a reaction to generate compound 2; (3) adding an ammonia source to a reaction solution of compound 2 to obtain compound 3 and compound 4; and (4) adding a second solvent and heating the resulting mixture for cyclization to obtain 2-hydroxy-3-fluoro-4-trifluoromethylpyridine. The present invention has low raw material cost and is a synthesis method, which has a short process cycle, is environmentally friendly, and is suitable for scale-up process production.

专利号:WO-2023128786-A1
优先权日:2021-12-30
标 题:New antiviral triazole derivatives, their synthesis and their use for treatment of mammalian viral infections

专利号:EP-4457218-A1
优先权日:2021-12-30
标题:New antiviral triazole derivatives, their synthesis and their use for treatment of mammalian viral infections

专利号:CN-117304094-A
优先权日:2023-09-21
标 题 :Synthesis method of 3-trifluoromethyl pyridine or 3-difluoro methyl pyridine compound