不对称1,3,2-苯并二氧磷杂环己烷非对映消旋体的合成及生物活性  

Synthesis and Biological Activity of Diastereomeric Racemates of Asymmetric 1, 3, 2-Benzodioxaphosphorin Derivatives

作　　者：成俊然[1] 文佳[1] 邵瑞链[1] 曹焕岩[1] 黄润秋[1] 

机构地区：[1]南开大学元素有机化学研究所

出　　处：《高等学校化学学报》1999年第9期1390-1393,共4页Chemical Journal of Chinese Universities

基　　金：天津市自然科学基金!983602711

摘　　要：通过相转移催化关环反应合成了新的6-取代-2-疏-2-烷（芳）氧-4-（2，-4二氯苯基）-4-氢-1，3，2-苯并二氧磷杂环已烷（3a－3g），用结晶法分离得到7对非对联消旋体，其结构经1HNMR、31PNMR和元素分析确证，化合物3a－A单晶X射线分析表明其构型为（2R，4S；Z2，4R）．生物活性测定结果表明，化合物3C有良好的杀虫活性，非对映消旋体A和B具有协同杀虫作用．New 6-substituted-2-alkoxy (aryloxy)-4- (2, 4-dichlorophenyl )-4H-1, 3, 2-benzodioxaphosphorin 2-sulfides 3a-3g were synthesized utilizing PTC cyclization reaction. Seven couples of compounds 3a-3g diastereomeric racemates (A and B) were separated by crystallization. Their structures were confirmed by 1H NMR, 31P NMR and elementary analysis.The single-crystal X-ray analysis of 3a-A indicated that its relative configuration is (2R,4S;2S, 4R). The preliminary bioassays indicate that compound 3c has a good insecticide activity. The diastereomeric racemates A and B show a synergistic insecticide activity.

关 键 词：苯并 二氧磷杂环己烷 非对映消旋体 生物活性 

分 类 号：O626.4[理学—有机化学] TQ450.2[理学—化学]