Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Institute of Biochemistry and Molecular Biology, Lanzhou University, Lanzhou, 730000, China.
Org Biomol Chem. 2013 Aug 28;11(32):5222-5. doi: 10.1039/c3ob41001c.
Herein, we have disclosed a catalytic asymmetric 1,5(6)-selective Michael/cyclization reaction of α-hydroxyimino cyclic ketones with γ,β-unsaturated α-keto esters. Unlike the previous catalytic strategies, this reaction provides a convenient 1,5(6)-selective asymmetric pathway to access synthetically useful ring-fused dihydropyrans. In general, high levels of yield, enantio- and diastereoselectivity (up to 99% yield, >99% ee and >20 : 1 dr) were obtained.
在这里,我们公开了一种催化不对称的 1,5(6)-选择性迈克尔/环化反应,涉及α-羟亚氨基环酮与γ,β-不饱和α-酮酯。与以前的催化策略不同,该反应提供了一种方便的 1,5(6)-选择性不对称途径,可获得合成有用的环合二氢吡喃。一般来说,获得了高产率、对映选择性和非对映选择性(高达 99%的产率、>99%的ee 值和>20 : 1 的 dr)。