Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (11): 1918-1924. Previous Articles     Next Articles

Original Articles

2-{2-[3-(取代苯基)-3-氧代-2-1,2,4-三唑-1-基-丙基]-苯基}-2-甲氧亚氨基乙酸甲酯和乙酰甲胺类衍生物的合成与杀菌活性研究

李国华 ; 杨 红*   

  1. (南京农业大学理学院 南京 210095)
  • 收稿日期:2008-02-04 修回日期:2008-05-05 发布日期:2008-11-18
  • 通讯作者: 杨 红

Synthesis and Antifungal Bioactivity of 2-{2-[3-(Subsititued phenyl)- 3-oxo-2-1,2,4-triazol-1-yl-propyl]-phenyl}-[2-methoxyimino]-acetic Acid Methyl Ester and N-Methyl-acetamide Derivatives

LI, Guo-Hua; YANG, Hong*   

  1. (College of Science, Nanjing Agricultural University, Nanjing 210095)
  • Received:2008-02-04 Revised:2008-05-05 Published:2008-11-18
  • Contact: YANG, Hong

Twenty-two 2-{2-[3-(subsititued phenyl)-3-oxo-2-1,2,4-triazol-1-yl-propyl]-phenyl}-[2-metho-
xyimino]-acetic acid methyl ester and {2-[3-(subsititued phenyl)-3-oxo-2-1,2,4-triazol-1-yl-propyl]- phenyl}-[2-methoxyimino]-N-methyl-acetamide derivatives were synthesized by reaction of methyl 2-methylbenzoylformate with hydrochloric acid salt of methoxyamine, methylamine, NBS and sodium 1H-1,2,4-triazolyl. The structures of the target compounds were characterized by IR, 1H NMR and mass spectra. These compounds at 10 µg•mL-1 were tested in vitro against five pathogenic fungi, Sclerotonia, Botrytis cinerea Pers, Gibberella zeae, Rhizoctorua solani and Pyricularia oryzae. The compounds Ha4, Ha5 and Ha7 showed potent antifungal activities against Sclerotonia, Ha2 and Hb8 showed potent antifungal ac-tivities against Rhizoctorua solani, Hb4 potent antifungal activities against Botrytis cinerea Pers, Hb4 and Hb5 potent antifungal activities against Gibberella zeae and Rhizoctorua solani.

Key words: 2-methoxyimino-2-phenylacetic acid derivative, synthesis, antifungal activity, 1H-1,2,4-triazole