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Copper-Catalyzed Asymmetric Hydrosilylation of β-Nitroethyl Aryl Ketones.
Organic Letters ( IF 4.9 ) Pub Date : 2020-01-09 , DOI: 10.1021/acs.orglett.9b04339
Weijun Zeng 1 , Xuefeng Tan 1 , Yang Yu 1 , Gen-Qiang Chen 1, 2 , Xumu Zhang 1
Affiliation  

A copper-catalyzed asymmetric hydrosilylation of β-nitroethyl aryl ketones has been disclosed, and the corresponding chiral alcohols could be obtained in high yields (up to 99% yield) and excellent enantioselectivities (up to 96% ee). Moreover, the reaction worked well on a gram scale with 0.3 mol % of ligand loading, indicating that our protocol has potential applications in the synthesis of important pharmaceuticals such as Tranylcypromine and Ticagrelor.

中文翻译:

铜催化的β-硝基乙基芳基酮的不对称氢化硅烷化。

已经公开了铜催化的β-硝基乙基芳基酮的不对称氢化硅烷化,并且可以以高收率(高达99%收率)和优异的对映选择性(高达96%ee)获得相应的手性醇。此外,该反应在0.3摩尔%的配体负载下以克为单位进行了良好的反应,表明我们的方案在合成重要药物(如Tranylcypromine和Ticagrelor)中具有潜在的应用。
更新日期:2020-01-10
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