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β-羰基膦酸酯是一类重要的有机化合物和反应中间体,在有机合成及药物化学中发挥着重要的作用.提供了一种高原子经济性、高选择性、温和的炔基膦酸酯水合反应体系.实验结果表明:在阳离子金催化剂(2.5 mol%)的催化作用下,以1,2-二氯乙烷(1 m L)为溶剂,室温下炔基膦酸酯(1 mmol)与水(3 mmol)发生水合反应,高收率、高区域选择性地得到β-羰基膦酸酯化合物(收率≥92%).该方法具有底物适用范围广、反应条件温和、环境友好等优点,为含β-羰基膦酸酯结构单元的天然产物及复杂药物分子的合成提供了一种新途径.
β-Carbonyl Phosphonates is an important class of organic compounds and reaction intermediates, and plays an important role in organic synthesis and pharmaceutical chemistry. It provides a high atomic economy, high selectivity and mild alkynylphosphonic acid Ester hydration reaction system.The experimental results show that alkynyl phosphonate (1 mmol) is reacted with 1,2-dichloroethane (1 m L) under the catalysis of cationic gold catalyst (2.5 mol%), ) Hydrate with water (3 mmol) to obtain β-carbonyl phosphonate compound with high yield and high selectivity (yield ≥92%). This method has the advantages of wide application range, mild reaction conditions, Friendly and other advantages for the synthesis of β-carbonyl phosphonate structural units of natural products and complex drug molecules provides a new way.