摘要/Abstract

成功开发了一种简便、有效地由铜催化"一锅法"合成2-苄基-3，4-二氢异喹啉-1-酮类化合物的方法.该方法以四氢异喹啉、苄基叠氮、含取代基的苯甲醛为原料，经过亲核加成并进一步氧化反应，一锅法合成目标化合物，且目标化合物产率为50%~70%.同时，进一步探究了催化剂的种类、添加剂的种类、反应温度、投料比等因素对反应的影响.结果表明，在CuCl₂为催化剂，CH₃COOH为添加剂，甲苯为溶剂的条件下，可高效地得到一系列2-苄基-3，4-二氢异喹啉-1-酮类化合物.
关键词: 氯化铜, 一锅法, 2-苄基-3,4-二氢异喹啉-1-酮
An facile, effective, copper-catalyzed one-pot approach to 2-benzyl-3,4-dihydroquinolin-1-ones has been successfully developed. The compounds were achieved by the reaction of tetrahydroisoquinoline, benzyl azide and benzaldehyde in one-pot fashion via nucleophilic addition reaction followed by oxidation. The desired products were afforded in the high yield of 50%~70%. Moreover, The effects of different catalyst, additives, reaction temperature and proportion of substrates on the reaction were also investigated. The results showed that the optimizing conditions of reaction were CuCl₂ as catalyst, CH₃COOH as additive and toluene as solvent. A series of 2-benzyl-3, 4-dihydro-2H-isoquinolin-1-ones can be efficiently obtained under the optimizing conditions.
Key words: CuCl₂, one-pot, 2-benzyl-3,4-dihydro-2H-isoquinolin-1-ones


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