4-氨基-5-氰基-6-烷胺基吡啶衍生物的合成与生物活性

Synthesis and Biological Activity of 4-Amino-5-cyano-6-alkylamino Pyridine Derivatives

采用六水合硝酸锌作催化剂、少量的乙醇钠为助催化剂,使用无水乙醇作为溶剂,将2-氰基-3-烷胺基-3-氨基-丙烯腈(N,N-缩醛)与β-二羰基化合物一步关环生成了一系列目标化合物4-氨基-5-氰基-6-烷胺基吡啶衍生物.通过1H NMR,IR,EI-MS,元素分析等方法对所合成的化合物进行了结构表征.代表化合物2-甲基-4-氨基-5-氰基-6-乙醇胺基-3-乙氧羰基吡啶经单晶X衍射证实了结构.对合成的多取代吡啶衍生物化合物作了初步的农药活性测试,测试结果表明:所合成的多取代吡啶衍生物部分化合物表现出较好的杀菌活性,同时也对油菜和稗草具有一定的除草活性.

A series of new 4-amino-5-cyano-6-alkylamino pyridine derivatives have been designed and synthesized from2-cyano-3-alkylamino-3-amino acrylonitriles and β-dicarbonyl compounds using Zn（NO3）2 and C2H5 ONa as catalysts in anhydrous ethanol. The structures of target compounds have been confirmed by 1H NMR, EI-MS, IR spectroscopy and elemental analysis. The structure of 2-methyl-4-amino-5-cyano-6-（2-hydroxyl ethylamino）-nicotinic ethyl ester has been determined by single crystal X-ray diffraction. The results of preliminary bioassay indicated that some compounds possess potential good fungicidal activities at a dosage of 5.0×10-5 g/m L, and some compounds also possess moderate herbicidal activities against the Rape and Barnyard grass.