Zhang Bangzhi, Han Fengxia, Wang Linqing, Li Dan, Yang Dongxu, Yang Xiaoli, Yang Junxian, Li Xiaofang, Zhao Depeng, Wang Rui
School of Life Sciences, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, Lanzhou, 730000 (China).
Chemistry. 2015 Nov 23;21(48):17234-8. doi: 10.1002/chem.201503105. Epub 2015 Oct 14.
The asymmetric Michael reaction between 5H-oxazol-4-ones and α,β-unsaturated acyl imidazoles is reported. A novel 2-benzo[b]thiophenyl-modified chiral ProPhenol species is synthesized and used as a ligand, leading to good enantioselectivities in this asymmetric conjugate addition reaction. Furthermore, the introduction of phenol additives as achiral co-ligands is found to improve the reaction's chemical yields, diastereoselectivities, and enantioselectivities.
报道了5H-恶唑-4-酮与α,β-不饱和酰基咪唑之间的不对称迈克尔反应。合成了一种新型的2-苯并[b]噻吩基修饰的手性ProPhenol配体，并将其用于该不对称共轭加成反应中，获得了良好的对映选择性。此外，发现引入酚类添加剂作为非手性共配体可提高反应的化学产率、非对映选择性和对映选择性。
