新手性N-苄氧甲酰基氨基酸芳基酯的微波合成和生物活性研究

Microwave Synthesis and Bioactivity of Novel Chiral Benzyloxycarbonylamino Acid Aryl Esters

用N,N'-二环己基碳二亚胺作脱水剂,在微波辐射条件下,N-苄氧甲酰基氨基酸和酚缩合反应生成了一系列新的N-苄氧甲酰基氨基酸芳基酯,缩短了反应时间。目标化合物的结构经1HNMR,13CNMR,IR和MS等进行了表征。对所合成的目标化合物进行了初步的生物活性测试,结果表明目标化合物具有一定的杀虫活性和杀菌活性,杀菌活性高于杀虫活性。

Under microwave irradiation, a series of novel aryl esters of N-Cbz-amino acids were synthesized in moderate yields by condensation reactions of N-Cbz-amino acids with substituted phenols in the presence of DCC and pyridine, but the reaction time was greatly shortened. The target products were characterized by ^1H NMR, ^13C NMR, IR and MS. A preliminary bioactivity study of the target products against organisms was investigated. The results showed they exhibited some fungicidal and insecticidal activities, and the activity against the phytopathogens was higher than against pest insects.