An efficient melting method for the synthesis of β-indole derivatives via Yonemitsu reaction was developed successfully using aldehyde, indole and Meldrum's acid as the starting materials and 50 μL water as green promoter without other solvent. A series of 5-[(indole-3-yl)-arylmethyl]-2,2-dimethyl-1,3-dioxane-4,6-dione derivatives were synthesized in 55%～ 94% yields. The remarkable advantages of this reaction were mild reaction condition, easy operation, tolerant the substrates with diverse functional groups and environment-friendly. Keywords melting method; multicomponent reaction; water; β-indole derivatives; green chemistry 吲哚骨架是广泛存在于天然产物和药物分子中的 重要结构单元 [1,2] , 特别是 β-取代吲哚衍生物, 已用于构 筑许多重要天然产物和具有生物活性的化合物骨架, 因 此, 其合成方法的研究格外引人注目 [3]. 由醛、 吲哚和麦 氏酸(Meldrum's acid)发生的三组分 Yonemitsu 缩合反应 是有效地合成 β-取代吲哚衍生物的方法之一 [4～11]. 近年 来, 报道了许多反应体系可以促进 Yonemitsu 缩合反应, 例如: 无催化剂条件下乙醇溶液中的反应 [12] 、无催化剂 无溶剂的固相研磨反应 [13] 、在生物质葡萄糖酸水溶液中 反应 [14] 和在新型反应介质低共熔溶剂中的反应 [15] 等.

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