CAS: 675590-04-2; 3-Bromo-5-(4-Fluorophenyl)Pyridine

相似化合物

142137-17-5 4422-32-6 1276123-21-7

上下游产品

3,5-dibromopyridine 4-fluoroboronic acid

📜3,5-二溴吡啶,4-氟苯硼酸置于四(三苯基膦)钯,Sodium Carbonate体系中,用 乙醇,水,甲苯 作为反应溶剂,以66%的收率获得产物3-溴-5-(4-氟苯基)吡啶
参考文献:Fine-Tuning The Selectivity Of Aldosterone Synthase Inhibitors: Structure−activity And Structure−selectivity Insights From Studies Of Heteroaryl Substituted 1,2,5,6-Tetrahydropyrrolo[3,2,1-Ij]Quinolin-4-One Derivatives
标题:Fine-Tuning The Selectivity Of Aldosterone Synthase Inhibitors: Structure−activity And Structure−selectivity Insights From Studies Of Heteroaryl Substituted 1,2,5,6-Tetrahydropyrrolo[3,2,1-Ij]Quinolin-4-One Derivatives
摘要:Pyridine Substituted 3,4-Dihydro-1H-Quinolin-2-Ones (E.G.,1-3) Constitute A Class Of Highly Potent And Selective Inhibitors Of Aldosterone Synthase (Cyp11B2),A Promising Target For The Treatment Of Hyperaldosteronism,Congestive Heart Failure,And Myocardial Fibrosis. Among These,Ethyl-Substituted 3 Possesses High Selectivity Against Cyp1A2. Rigidification Of 3 By Incorporation Of The Ethyl Group Into A 5-Or 6-Membered Ring Affords Compounds With A Pyrroloquinolinone Or Pyridoquinolinone Molecular Scaffold (E.G.,4 And 5). It Was Found That These Molecules Are Even More Potent And Selective Cyp11B2 Inhibitors Than Their Corresponding Open-Chain Analogues. Moreover,Pyrroloquinolinone 4 Exhibits No Inhibition Of The Six Most Important Hepatic Cyp Enzymes As Well As A Bioavailability In The Range Of The Marketed Drug Fadrozole. The Sar Studies Disclose That Subtle Changes In The Heterocyclic Moiety Are Responsible For Either A Strong Or A Weak Inhibition Of The Highly Homologous 11 Beta-Hydroxylase (Cyp11B1). These Results Are Not Only Important For Fine-Tuning The Selectivity Of Cyp11B2 Inhibitors But Also For The Development Of Selective Cyp11B1 Inhibitors That Are Of Interest For The Treatment Of Cushing'S Syndrome And Metabolic Syndrome.
DOI:10.1021/jm101470K