100-51-6 + 766-11-0 = 83664-33-9 反应条件:1.1 Reagents: Sodium Hydride Solvents: Tetrahydrofuran; 30 Min,0 °C1.2 Overnight,70 °C1.3 Reagents: Water 标题:Optimization Of Triarylpyridinone Inhibitors Of The Main Protease Of Sars-Cov-2 To Low-Nanomolar Antiviral Potency 作者:Zhang,Chun-Hui; Et Al 参考文献:Acs Medicinal Chemistry Letters 日期:2021 卷标:12(8) 页码:1325-1332]
1072-97-5 = 83664-33-9 反应条件:1.1 Reagents: Sulfuric Acid Solvents: Water; Rt -> 5 °C1.2 Reagents: Sulfuric Acid,Hydrogen Peroxide Solvents: Water; Overnight,Rt1.3 Reagents: Potassium Hydroxide Solvents: Water; Basified,Rt2.1 Reagents: Cesium Carbonate Catalysts: 1,10-Phenanthroline,Cuprous Iodide Solvents: Toluene; 24 H,110 °C 标题:A Simple Cu-Catalyzed Coupling Approach To Substituted 3-Pyridinol And 5-Pyrimidinol Antioxidants 作者:Nara,Susheel J.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2008 卷标:73(23) 页码:9326-9333]
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
参考标题:Synthesis Of Amido-N-Imidazolium Salts And Their Applications As Ligands In Suzuki-Miyaura Reactions: Coupling Of Hetero- Aromatic Halides And The Synthesis Of Milrinone And Irbesartan 作者:Manian Rajesh Kumar,Kyungho Park,Sunwoo Lee |发布日期:2010.12.17 摘要:Catalytic System Based On Palladium-Amido-N-Heterocyclic Carbenes For Suzuki-Miyaura Coupling Reactions Of Heteroaryl Bromides Is Described. A Variety Of Sterically Bulky, Amido-N-Imidazolium Salts Were Synthesized In High Yields From The Corresponding Anilines. This Catalytic System Effectively Promoted Suzuki-Miyaura Couplings Of Heteroaryl Bromides And Chlorides With A Range Of Boronic Acids To
合成参考文献
摘要:Spitzner, D., Science of Synthesis, (2005) 15, 176.