α-氰基丙烯酸酯类手性衍生物合成反应机理探讨

Synthesis and Mechanism of Chiral α-Cyanoacrylates Compounds

α-氰基丙烯酸酯类化合物是一类抑制植物光合作用PSⅡ重要除草剂,近年又有研究相继发现其抗癌、杀菌等活性,有重要研究意义,本文主要以3-对三氟甲基苯胺-3-[(R/S-)-α-甲基苄胺]-2-氰基丙烯酸酯及其中间体的合成为基础,对相应化合物及其中间体通过表征确定了其立体构型,对该反应的合成机理给出了相应合理的解释.同时,发现该类化合物具有一定抗烟草花叶病毒活性及抗癌活性,值得关注.

α - Cyanoacrylate is a kind of important herbicide targeted in Photosystem PSⅡ.Started from cyano ethyl acetate, the intermediate and the title compounds of Ethyl 3 - [ （R/S） - 1 -phenylethylamino ] -3 - （4 - （trifluoromethyl） -phenylamino） -2 -cyanoacrylate were synthesized. Also three of the title compounds were characterized through Single crystal diffraction and found to be E - isomerism,its reaction mechanism was given. It was also found that they possess high bioaetivity against TMV and PC3 cells in a certain extent.