6种阿魏酸酰胺类衍生物的合成及除草活性的测定

Synthesis of six ferulic acid amide derivatives and determination of herbicidal activity

为了获取更高除草活性的化合物,以阿魏酸的羧基进行酰胺化的改造,以三乙胺作为缚酸剂,DMF作为脱水剂,BOP(卡特缩合剂)为催化剂进行酰胺化反应,最终得到了6个阿魏酸的酰胺类衍生物。以反枝苋、稗草、马唐和油菜为供试植物,莠去津作为阳性对照,利用小杯法和茎叶喷雾法对6个化合物进行除草活性的测定。药物浓度设置为200 mg/L。小杯法的结果显示,化合物5、6对油菜的根具有抑制活性,抑制率分别为(73.96±6.09)%、(63.02±5.45)%。化合物6对稗草的茎抑制率为(63.46±7.68)%。在茎叶喷雾法的结果中化合物1~6均对稗草和马唐地上部具有抑制作用。其他化合物在对供试植物的小杯法和茎叶喷雾法的试验中均无明显的抑制作用或相反具有促进作用。

In order to obtain compounds with higher herbicidal activity,amidation of carboxyl groups of ferulic acid is carried out,triethylamine is used as an acid-binding agent,DMF is used as a dehydrating agent,and BOP（Carteses condensation agent）is used as a catalyst for amidation reaction.Six ferulic acid amide derivatives are obtaimed.Using Echinochloa crusgalli,Digitaria sanguinalis,Amaranthus retroflexus,Brassica napus as test plants.Atrazine as a positive control.The herbicidal activity of the 6 compounds is determined by the small cup method and stem-leaf spray method.The drug concentration is set to 200 mg/L.The results of the small cup method show that compounds 5 and 6 have inhibitory activity on the roots of B.napus,with inhibition rates of（73.96±6.09）% and（63.02±5.45）%.The inhibitory rate of compound 6 against E.crusgalli is（63.46±7.68）%.In the stem-leaf spray method,compounds 1-6 all have inhibitory effects on the E.crusgalli and D.sanguinalis.The other compounds have no obvious inhibitory effect on the test plants by the method of small cup and stem-leaf spray,or have the opposite promotion effect.