【摘要】 研究了一种在碳酸氢钠-二甲亚砜催化体系中,孕甾烯醇酮吡咯化合物及其制备方法,起始原料廉价易得,反应过程中条件温和,无特殊要求的装置,可适合产业化生产。该方法采用一锅法进行合成,中间体无需分离。其最佳反应条件为:常压,115℃,NH-孕甾烯醇酮吡咯(1),收率为41.9%;N-乙烯基孕甾烯醇酮吡咯(2),收率为30.3%。催化剂用量均以NaHCO3/mg∶DMSO/mL=425∶10为宜。产物IR及1 H NMR均与文献值一致。所得化合物对小麦赤霉病菌、辣椒枯萎病菌、苹果腐烂病菌具有抑制作用。在500μg/mL浓度下,所得化合物NH-孕甾烯醇酮吡咯(1)和N-乙烯基孕甾烯醇酮吡咯(2)对三种植物病原菌均有较好的抑制效果,抑制率均在80%以上,对小麦赤霉病原菌的抑制率更是达到了90%以上。可见,化合物1和2具有良好的抗植物病菌活性。更多还原

【Abstract】 The pregnenolone compounds were synthesized using NaHCO3-DMSO as catalyst.The raw materials can be acquired easily,and the reaction conductions were moderate.No special equipment was needed and the method was suited for industrial production.In this method one-pot synthesis reaction was adopted.The optimum reaction conditions were:normal pressure and 115℃.The NH-pregnenolone pyrrole(1)yield was 41.9%,while the N-vinyl pregnenolone pyrrole(2)yield was 30.3%.The amount of catalysts were NaHCO3 /mg∶DMSO/mL=425∶10.The results of IR and 1 H NMR of the products agreed with those in the literature.The products were used to restrain fusarium graminearum,fusarium oxysporum and cytospora mandshuric.In 500μg/mL concentration,NH-pregnenolone pyrrole(1)and N-vinyl pregnenolone pyrrole(2)had inhibition effect for the three kinds of plant pathogenic bacteria and the inhibition rate were above 80%,The inhibition rate for fusarium graminearum achieved above 90%.The compounds 1 and 2 had good anti plant bacteria activity.更多还原