一种手性β-氨基膦酸酯的合成方法研究

Study on the synthesis of a chiral β-amino phosphonate

  • 摘要: 合成了4种金鸡纳碱衍生的手性相转移催化剂,用于催化 (2-氧代丙基) 膦酸二甲酯与α-氨基砜的不对称Mannich反应制备β-氨基膦酸酯. 经过反应条件的优化,确定了−40 ℃,以化合物 D 为催化剂,甲苯为溶剂,6% LiOH水溶剂为碱的最佳反应条件,手性β-氨基膦酸酯衍生物的收率达到90%,ee值达到60%.

     

    Abstract: Four cinchona-derived chiral phase transfer catalysts were synthesized to catalytic asymmetric Mannich reaction of dimethyl (2-oxopropyl)phosphonate with α-aminosulfones to prepare β-aminophosphonates. After the optimization of the reaction conditions, the optimal reaction conditions were determined at −40 ℃, using compound D as the catalyst, toluene as the solvent, and 6% LiOH water solvent as the base, and the yield of chiral β-aminophosphonate derivatives reached 90%, the ee reached 60%.

     

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