CAS: 210963-61-4; 3-(2-Bromoethoxy)Benzonitrile

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m-cyanophenol 2-bromoethanol diethylazodicarboxylate ethylene dibromide

📜3-氰基苯酚,1,2-二溴乙烷 在 Potassium Carbonate,Potassium Iodide体系中,用 丁酮作为反应溶剂,反应 48.0H,以30%的收率获得3-(2-Bromoethoxy)Benzonitrile
参考文献:New Serotonin 5-Ht1A Receptor Agonists Endowed With Antinoiceptive Activity In Vivo
标题:New Serotonin 5-Ht1A Receptor Agonists Endowed With Antinoiceptive Activity In Vivo
摘要:We Report The Synthesis Of New Compounds 4-35 Based On Two Different Openings (A And B) Of The Chromane Ring Present In The Previously Identified 5-Ht1A Receptor (5-Ht1Ar) Ligand 3. The Synthesized Compounds Were Assessed For Binding Affinity,Selectivity,And Functional Activity At The 5-Ht1Ar Selected Candidates Resulting From B Opening Were Also Evaluated For Their Potential Antinoiceptive Effect In Vivo And Pharmacokinetic Properties In Vitro. Analogue 19 [2-(4-{[2-(2-Ethoxyphenoxy)Ethyl]Amino}Butyl)Tetrahydro-1H-Pyrrolo[1,2-C]Imidazole-1,3(2H)-Dione] Has Been Characterized As A High-Affinity And Potent 5-Ht1Ar Agonist (K-I = 2.3 Nm; Ec50 = 19 Nm). Pharmacokinetic Studies Indicated That Compound 19 Displays A Good Metabolic Stability In Human Liver Microsomes (T(1/2) Similar To 3 H And Clint = 3.5 Ml/Min/Kg,At 5 Mu M),And A Low Level Of Protein Binding (25%,At 5 Mu M). Interestingly,19 (3 Mg/Kg,Ip,And 30 Mg/Kg,Po) Caused Significant Attenuation Of Formalin-Induced Behavior In Early And Late Phases Of The Mouse Intradermal Formalin Test Of Pain,And This In Vivo Effect Was Reversed By The Selective 5-Ht1Ar Antagonist Way-100635. Thus,The New 5-Ht1Ar Agonist Identified In This Work,19,Exhibits Oral Analgesic Activity,And The Results Herein Represent A Step Toward Identifying New Therapeutics For The Control Of Pain.
Doi:10.1021/Jm400766K