2-(2-氟-3,4-二甲氧基苯基)乙腈置于sodium Hydroxide体系中,化学反应 16.0H,以27 G的收率获得产物4-氟-3-甲氧基苯乙酸
参考文献:Dopamine Agonists Related To 3-Allyl-6-Chloro-2,3,4,5-Tetrahydro-1-(4-Hydroxyphenyl)-1H-3-Benzazepine-7,8-Diol,6-Position Modifications
标题:Dopamine Agonists Related To 3-Allyl-6-Chloro-2,3,4,5-Tetrahydro-1-(4-Hydroxyphenyl)-1H-3-Benzazepine-7,8-Diol,6-Position Modifications
摘要:The N-Allyl Derivative (Sk&f 85174) Of 6-Chloro-2,3,4,5-Tetrahydro-1-(4-Hydroxyphenyl)-1H-3-Benzazepine-7,8-Diol (Sk&f 82526) Retains The Da-1 Agonist Potency Of The Latter Compound But Unlike The Parent Also Shows Substantial Da-2 Agonist Activity. In A Previous Study Of N-Substituted Benzazepines These Combined Agonist Effects Were Shown To Be Uniquely Associated With The N-Allyl Group. A Continuation Of This Research Has Examined Dependency Of Combined Da-2/da-1 Agonist Activities On 6-Position Modification With The Specific Objective Of Developing An Agonist With Maximum Effectiveness And Potency At The Da-2 Receptor Subtype. Da-2 Agonist Activity Was Measured In A Rabbit Ear Artery Assay,And Da-1 Agonist Activity Was Determined In An Adenylate Cyclase Assay. Replacing Chloro With Bromo Retains The Activity Pattern And The Potency Of The Chloro Compound; Replacement With A Hydrogen Causes A Decrease Of Both Da-1 And Da-2 Receptor Activating Potency. Introduction Of A 6-Methyl Group Causes Loss Of Da-2 Agonist Activity And Reduction In Da-1 Agonist Potency. Substitution With A 6-Fluoro Provides The Best Balance Of Da-2 And Da-1 Agonist Activities; This Compound Was Moderately Potent In Both Assays.
DOI:10.1021/jm00384A006