4-氨基苯乙酮置于cucl2*h2O 盐酸,Sodium Nitrite,二氧化硫体系中,用 水,溶剂黄146 用作溶剂,化学反应 2.0H,以55%的收率获得4-乙酰基苯磺酰氯
参考文献:Simple And Efficient Synthesis Of 3,4-Dihydro-2-Pyridones Via Novel Solid-Supported Aza-Annulation
标题:Simple And Efficient Synthesis Of 3,4-Dihydro-2-Pyridones Via Novel Solid-Supported Aza-Annulation
摘要:A Diverse Array Of 3,4-Dihydro-2-Pyridones 13 Were Produced Utilizing The Unique Properties Of Solid-Supported Reactions To Both Drive The Reactions To Completion And Isolate The Desired Products. The Pyridones Were: Synthesized In High Purity By A Simple Sequence Of Navel Steps Commencing From An Acetophenone-Functionalized Resin. The Para-Substituted Acetophenone 9 Could Be Anchored To The Resin Through Either A Sulfonamide Or A Carboxamide Linkage. The Sulfonamide Resin 9A,Which Gave The Best Results,Was Treated With Several Aryl Aldehydes And Ethoxide To Give A Variety Of Chalcones 10A-K,In Excellent Yield (82-99%) Upon Tfa Cleavage. Addition Of Either Methyl Or Allyl Malonate And Dbu To 10A-K Afforded Smoothly The Michael Adducts 11A-J (70-99%) Which Were Subsequently Cyclized In One Step Employing Acetic Acid As A Catalyst And Several Diverse Amines To Give Pure 3,4-Dihydro-2-Pyridones 13A-P In Moderate To Excellent Yields (30-98%).
Doi:10.1021/jo005609X