N-[(2-Chlorophenyl)Methylene]-2,2-Dimethoxyethanamine置于硫酸体系中,化学反应 0.5H,反应生成 8-氯异喹啉
参考文献:Inhibitors Of Phenylethanolamine N-Methyltransferase And Epinephrine Biosynthesis. 1. Chloro-Substituted 1,2,3,4-Tetrahydroisoquinolines
标题:Inhibitors Of Phenylethanolamine N-Methyltransferase And Epinephrine Biosynthesis. 1. Chloro-Substituted 1,2,3,4-Tetrahydroisoquinolines
摘要:In A Search For Inhibitors Of Epinephrine Biosynthesis As Potential Therapeutic Agents,A Series Of 13 Ring-Chlorinated 1,2,3,4-Tetrahydroisoquinolines Was Prepared. These Compounds Were Tested Initially For Their Ability To Inhibit Rabbit Adrenal Phenylethanolamine N-Methyltransferase (Pnmt) In Vitro. Enzyme-Inhibitor Dissociation Constants,Determined For The Six Most Potent Members Of The Series,Indicated The Following Order Of Decreasing Potency: 7,8-Cl2 Greater Than 6,7,8-Cl3 Greater Than 7-Cl Approximately 5,6,7,8-Cl4 Greater Than 5,7,8-Cl3. These Compounds Were Subsequently Examined For Pnmt-Inhibiting Activity In Intact Rats And Mice. 7,8-Dichloro-1,2,3,4-Tetrahydroisoquinoline (13,Sk&f 64139) Was The Most Potent Member Of The Series Both In Vitro And In Vivo And Is Currently Undergoing Clinical Investigation.
DOI:10.1021/jm00179A007