论文部分内容阅读
Angew.Chem.Int.Ed.2016,55,331~335含有手性的磺酰基化合物在医药和工业上具有广泛的应用价值,不对称合成手性磺酰基化合物历来被广大化学家所关注.近期,重庆大学创新药物研究中心闫海龙课题组通过手性开环冠醚催化剂催化的不对称β-消除反应,首次实现了β-砜酮的动力学拆分.该反应的机理可以解释为R构型开环冠醚催化剂选择性地脱去S构型底物中的磺酰基团,使S构型底物生成查尔酮类化合物的速率远高于R构型底物发生β-消除生成查尔酮的速率,实现了消旋体磺
Angew.Chem.Int.Ed.2016,55,331 ~ 335 Chiral sulfonyl compounds have a wide range of applications in medicine and industry, asymmetric synthesis of chiral sulfonyl compounds has always been the majority of chemists concerned.Recently, Chongqing Yan Hailong, a research group at the Center for Innovative Drug Research, for the first time, catalyzed the asymmetric β-elimination reaction catalyzed by a chiral ring-opened crown ether catalyst, which led to the kinetic resolution of β-sulfone ketones for the first time.The mechanism of this reaction can be explained by the R configuration The cyclic ether catalyst selectively removes the sulfonyl groups in the S-type substrate, so that the rate of formation of the chalcone-type compound by the S-type substrate is much higher than that of the R-type substrate by β-elimination to yield chalcone Of the rate of racemic sulfonates