Chen Wei, Zhou Zhao-Hui, Chen Hong-Bin
Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, P. R. China.
Org Biomol Chem. 2017 Feb 7;15(6):1530-1536. doi: 10.1039/c6ob02569b.
Chiral β-amino alcohol ligands were found effective for the copper(ii)-catalyzed asymmetric Henry reaction of benzofuran-2-carbaldehydes with nitromethane, which led to the formation of (S)-enriched benzofuryl β-nitro alcohols with satisfactory enantioselectivities (up to 98% ee). Using this catalytic protocol, bioactive (S)-benzofuryl β-amino alcohols could be conveniently prepared in short steps.
发现手性β-氨基醇配体对铜（II）催化的苯并呋喃-2-甲醛与硝基甲烷的不对称亨利反应有效，该反应导致形成对映体选择性良好（高达98%ee）的富含（S）的苯并呋喃基β-硝基醇。使用这种催化方法，可以通过简短步骤方便地制备具有生物活性的（S）-苯并呋喃基β-氨基醇。
