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

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;2S,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.     

Crystal Structure of Ethoxyethyl 3-(2-Chloro-5-pyridyl methylamino)-2-cyano-4-methylpent-2-enoate

1 INTRODUCTION The nature and topography of the herbicide binding site in the reaction center of photosystem Ⅱ (PSⅡ) have been the subject of intense interest for many years. Among several commercially important herbicides with different structures such as atrazine and polypeptide of the PSII reaction center[1], the cyanoacrylates with general structure 1 have proved hightly potent and useful as probes[2, 3] of the receptor because their activities as inhibitors of photosynthetic ele…