A new solvent-free microwave-assisted procedure for the Petasis multicomponent reaction was developed. This method is the first application of the borono-Mannich reaction in solvent-free conditions and proved its applicability to various boronic acids and secondary amines. Results are very good in term of yields with shorter reaction time than the classical methods. Because of the efficiency of the method, full conversion of the starting materials towards the expected product was achieved, starting from stoichiometric quantities of reactants, avoiding the usual solvent-consuming column chromatography on silica gel. No purification step other than an aqueous washing was required.
一种新的无溶剂微波辅助Petasis多组分反应方法被开发出来。这种方法首次将
硼-曼尼希反应应用于无溶剂条件,并证明其适用于各种
硼酸和仲胺。与传统方法相比,该方法反应时间短,收率很高。由于该方法效率高,从
化学计量量的反应物开始,起始原料就能完全转化为预期产物,避免了通常在
硅胶上进行耗溶剂的柱色谱法。除了
水冲洗外,不需要其他纯化步骤。