吡唑并嘧啶-4-酮衍生物的合成与除草活性  

Synthesis and Herbicidal Activities of Pyrazolo[3,4-d]pyrimidin-4-one Derivatives

作　　者：刘惠[1] 王宏青[1,2] 刘钊杰[1] 

机构地区：[1]华中师范大学化学学院,武汉430079 [2]南华大学化学化工学院衡阳

出　　处：《应用化学》2005年第3期286-290,共5页Chinese Journal of Applied Chemistry

基　　金：科技部国家"九五"重点攻关项目(97 563 02 05)

摘　　要：研究了膦亚胺(4)与芳基异氰酸酯、取代酚的连续aza -Wittig和关环反应合成 1 -苯基- 3- 甲硫 (砜 )基 -5 -取代芳基- 6- (4- (2 烷氧羰基)乙氧基)苯氧基吡唑[3, 4 -d]并嘧啶- 4- 酮类化合物的方法,其产物结构经元素分析、1HNMR、EI -MS和IR确证。初步生物活性测试表明,该类化合物对单子叶和双子叶的根的生长具有较好的抑制活性。如浓度为 100mg/L时,化合物 6h、7a、7c对油菜根和稗草根的抑制率均超过 90%。Phenyl-3-methylthio(methanesulfonyl)-5-substituted aryl 6-(4-(2-alkoxy carbonyl) ethoxy)phenoxypyrazolo\pyrimidin-4-one derivatives( 6 and 7) were synthesized by a tandem aza-Wittig and annulation reaction of iminophosphorance 4 with aromatic isocyanate and substituted phenol s. The structures of all the target compounds have been confirmed. The preli minary bioassay tests indicate that compounds 6h, 7a, 7c possess h igh herbicidal activities against the roots of rape and barnyard grass. Their inhibitory rates against the roots of rape and barnyard grass are more than 90 %.

关 键 词：吡唑[3 4-d]并嘧啶酮 苯氧丙酸酯 AZA-WITTIG反应 合成 除草活性 

分 类 号：O621[理学—有机化学] TQ226.3[理学—化学]