Synthesis and Insecticidal Structure-Activity Relationships of Novel Tonghaosu Analogs  

作　　者：尹标林 陈立 徐汉虹 胡泰山 吴毓林 

机构地区：[1]State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China [2]Laboratory of Insect Toxicology, South China Agricultural University, Guangzhou, Guangdong 510642, China

出　　处：《Chinese Journal of Chemistry》2006年第2期240-246,共7页中国化学（英文版）

基　　金：Project supported by the National Natural Science Foundation of China （Nos. 29672083, 20072043）, the Chinese Academy of Sciences, the Ministry of Science and Technology of China （No. G2000077502）, and the Shanghai Commission of Science and Technology.

摘　　要：Twenty-one tonghaosu analogs were synthesized via hydroamination or selective reduction of the endocyclic double bond of the corresponding dienol spiroketals. Structures of all the new compounds were confirmed by ^1H NMR, IR, MS, HREIMS or elemental analysis. Their antifeedant activity against large white butterfly （Pieris brassicae L） and larvicidal activity toward mosquito （Culex quinquefasciatus Say） were examined. Some of them exhibited antifeeding activities comparable to or stronger than tonghaosu Z-1. Based on the activity data, the preliminary structure-activity relationship was also discussed, which might be instructive for finding out lead compounds with better bioactivities in the future.Twenty-one tonghaosu analogs were synthesized via hydroamination or selective reduction of the endocyclic double bond of the corresponding dienol spiroketals. Structures of all the new compounds were confirmed by ^1H NMR, IR, MS, HREIMS or elemental analysis. Their antifeedant activity against large white butterfly （Pieris brassicae L） and larvicidal activity toward mosquito （Culex quinquefasciatus Say） were examined. Some of them exhibited antifeeding activities comparable to or stronger than tonghaosu Z-1. Based on the activity data, the preliminary structure-activity relationship was also discussed, which might be instructive for finding out lead compounds with better bioactivities in the future.

关 键 词：spiroketal  hydroamination  reduction  antifeedant  insecticidal  Pieris brassicae Culex quinquefasciatus 

分 类 号：TQ453[化学工程—农药化工]