CAS: 5001-96-7; 2-(2-Fluoro-[1,1'-Biphenyl]-4-yl)Acetic Acid

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CAS号1393566-55-6 2--(2--fluoro--... | CAS号57592-43-5 2-氟联苯基-4-甲醛 | CAS号216701-21-2 (2-氟联苯-4-基)甲醇 | CAS号108-86-1 溴苯 | CAS号352-70-5 3-氟甲苯 | CAS号127425-73-4 3-氟-4-溴溴苄 | CAS号499983-13-0 3-氟-4-溴苯乙腈 | CAS号452-74-4 3-氟-4-溴甲苯 | CAS号124-38-9 二氧化碳 | CAS号69168-29-2 2-氟-4-甲基-1,1'-联苯 | CAS号5104-49-4 氟比洛芬

📜4-溴-3-氟甲苯置于n-溴代丁二酰亚胺(Nbs),四丁基溴化铵,双氧水,Palladium Diacetate,Sodium Carbonate,Potassium Carbonate,过氧化苯甲酰体系中,用 四氯化碳,乙醇,水,二甲基亚砜 作为反应溶剂,化学反应 3.0H,反应生成 2-氟联苯-4-乙酸
参考文献:Inhibition Of Amyloidogenesis By Nonsteroidal Anti-Inflammatory Drugs And Their Hybrid Nitrates
标题:Inhibition Of Amyloidogenesis By Nonsteroidal Anti-Inflammatory Drugs And Their Hybrid Nitrates
摘要:Poor Blood-Brain Barrier Penetration Of Nonsteroidal Anti-Inflammatory Drugs (Nsaids) Has Been Blamed For The Failure Of The Selective Amyloid Lowering Agent (Sala) R-Flurbiprofen In Phase 3 Clinical Trials For Alzheimer'S Disease (Ad). No-Donor Nsaids (No-Nsaids) Provide An Alternative,Gastric-Sparing Approach To Nsaid Salas,Which May Improve Bioavailability. Nsaid Analogues Were Studied For Anti-Inflammatory Activity And For Sala Activity In N2A Neuronal Cells Transfected With Human Amyloid Precursor Protein (App). Flurbiprofen (I) Analogues Were Obtained With Enhanced Anti-Inflammatory And Antiamyloidogenic Properties Compared To I,However,Esterification Led To Elevated A Beta(1-42) Levels. Hybrid Nitrate Prodrugs Possessed Superior Anti-Inflammatory Activity And Reduced Toxicity Relative To The Parent Nsaids,Including Clinical Candidate Chf5074. Although Hybrid Nitrates Elevated A Beta(1-42) At Higher Concentration,Sala Activity Was Observed At Low Concentrations (<= 1 Mu M): Both A Beta(1-42) And The Ratio Of A Beta(1-42)/a Beta(1-40) Were Lowered. This Biphasic Sala Activity Was Attributed To The Intact Nitrate Drug. For Several Compounds,The Selective Modulation Of Amyloidogenesis Was Tested Using An Immunoprecipitation Maldi-Tof Approach. These Data Support The Development Of No-Nsaids As An Alternative Approach Toward A Clinically Useful Sala.
DOI:10.1021/jm101450P

专利信息

专利号:WO-2024130689-A1
优先权日:2022-12-23
标 题:2-fluorobiphenyl-4-acetic acid derivative, preparation method therefor, and use thereof
发明人：CHEN YUXIN; CHEN MINGXIA; YAO WENJUN
权利人:JIANGSU PROTELIGHT PHARMACEUTICAL & BIOTECHNOLOGY CO LTD
摘要:Disclosed are a 2-fluorobiphenyl-4-acetic acid derivative, a preparation method therefor, and use thereof. The structural formula of the 2-fluorobiphenyl-4-acetic acid derivative is set forth in formula I. The compound can be prepared by means of an artificial synthesis method, having a broad-spectrum anti-tumor effect, prolonging the survival period of tumor patients and improving their survival quality. The compound has stable therapeutic effects, low toxicity and easy acceptance by a human body, and is applicable to the treatment of most cancers, thus exhibiting certain advantages over currently available anti-tumor drugs.