三组分一锅法合成3,4-二氢喹唑啉衍生物

One-Pot Three-Component Synthesis of 3,4-Dihydroquinazoline Derivatives

提出了一种通过偶氮二甲酸二乙酯(DEAD)促进的氧化Ugi/氮杂Wittig反应合成3,4-二氢喹唑啉的新方法.该方法应用膦亚胺5与N-芳基-1,2,3,4-四氢异喹啉6和羧酸7在DEAD存在下发生串联氧化型Ugi/氮杂Wittig反应,以中等到良好的产率生成3-(四氢异喹啉-1-甲酰基)取代的3,4-二氢喹唑啉8.

A new one-pot synthesis of 3,4-dihydroquinazolines by diethyl azodicarboxylate(DEAD)-promoted oxidative Ugi/aza-Wittig reaction was developed.The reactions of iminophosphoranes 5,N-aryl-1,2,3,4-tetrahydroisoquinolines 6 and acids 7 produced 3-(tetrahydroisoquinolin-1-formyl)substituted 3,4-dihydroquinazolines 8 in moderate to good yields in the presence of DEAD by tandem oxidative Ugi/aza-Wittig reaction.