结合药物设计原理,对前期研究的活性结构类型进行优化.在超声辐射下,以α-羟基膦酸酯、苯磺酰氯为原料设计合成系列新型O,O’-二烷基-α-取代苯基-α-苯磺酰氧基甲基膦酸酯衍生物,考察不同溶剂、反应温度、反应时间、反应功率对产率的影响,得到最佳反应条件.该方法简便可行、时间较短、产率较高.目标物结构经1H NMR,IR,MS及元素分析确认,并研究了质谱裂解规律.初步生物活性测试表明:部分目标物对肿瘤细胞A-549有较好的抑制作用. Based on the principle of drug design, the types of active structures in the previous studies were optimized.A series of novel O, O’-dialkyl-α-substituted benzenes were designed and synthesized by using α-hydroxy phosphonate and benzenesulfonyl chloride as raw materials under ultrasonic irradiation The effects of different solvents, reaction temperature, reaction time and reaction power on the yield were investigated and the optimal reaction conditions were obtained.The method was simple and feasible, with shorter time, And the yield was high.The structures of the target compounds were confirmed by 1H NMR, IR, MS and elemental analysis, and the cleavage regularity of mass spectrometry was studied.The preliminary biological activity tests showed that some of the target compounds had a good inhibitory effect on A-549 tumor cells.