N-(2,6-二甲苯基)-N-酰基丙氨酸甲酯类化合物的合成及生物活性研究

Synthesis and Bioactivity of N-(2,6-xylyl)-N-acylalanines

以α-氯丙酸为起始原料,甲酯化后得α-氯丙酸甲酯;在碘化钾催化下,α-氯丙酸甲酯与2,6-二甲基苯胺缩合获得中间体N-(2,6-二甲苯基)丙氨酸甲酯,再在室温下以吡啶作缚酸剂,与系列羧酸酰氯反应15 h,合成了12个新型N-(2,6-二甲苯基)-N-酰基丙氨酸甲酯类目标化合物。目标化合物的结构经GC-MS、FTIR和元素分析确认。对目标化合物进行了杀菌、杀虫、除草生物活性测定,结果表明,各化合物均具有不同程度的杀菌生物活性。

Methyl α-chloropropionate was prepared from α-chloropropinic acid and methanol at first, and then reacted with 2,6-dimethylaniline in the presence of potassium iodide to give N-（2,6-xylyl） alanine methyl ester, which, by acylation with different acyl chlorides at normal temperature with pyridine as acid scavenger, gave 12 new N-（2,6-xylyl）-N-acylalanine methyl esters. According to the screening procedure of these new compounds, the insecticidal, herbicidal and fungicidal bioactivity tests were taken. The results show that some of these N-（2,6-xylyl）-N-acylalanine methyl esters have high fungicidal activity.