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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
引用本文:许栋梁,唐子龙,刘汉文,陈卫文,欧晓明. 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[J]. 精细化工中间体, 2008, 38(3)
作者姓名:许栋梁  唐子龙  刘汉文  陈卫文  欧晓明
作者单位:湖南科技大学,化学化工学院,分子构效关系湖南省高校重点实验室,湖南,湘潭,411201;湖南化工研究院国家农药创制工程技术研究中心,湖南,长沙,410007
基金项目:教育部留学回国人员科研启动基金 , 湖南省自然科学基金 , 湖南省社会科学基金
摘    要: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。

关 键 词:氨基酸  氨基酸芳基酯  微波合成  生物活性

Microwave Synthesis and Bioactivity of Novel Chiral Benzyloxycarbonylamino Acid Aryl Esters
XU Dong-liang,TANG Zi-long,LIU Han-wen,CHEN Wei-wen,OU Xiao-ming. Microwave Synthesis and Bioactivity of Novel Chiral Benzyloxycarbonylamino Acid Aryl Esters[J]. Fine Chemical Intermediates, 2008, 38(3)
Authors:XU Dong-liang  TANG Zi-long  LIU Han-wen  CHEN Wei-wen  OU Xiao-ming
Abstract: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.
Keywords:amino acid  amino acid aryl ester  microwave synthesis  bioactivity
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