School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.
J Org Chem. 2012 Jan 6;77(1):612-6. doi: 10.1021/jo202204j. Epub 2011 Dec 6.
Various substituted aryl-pyridyl ketones were hydrogenated in the presence of Ru-XylSunPhos-Daipen bifunctional catalytic system with enantiomeric excesses up to 99.5%. Upon introduction of a readily removable ortho-bromo atom to the phenyl ring, enantiomerically enriched 4-chlorophenylpyridylmethanol was obtained by hydrogenation method with 97.3% ee, which provided an important chiral intermediate for some histamine H(1) antagonists.
各种取代的芳基-吡啶基酮在 Ru-XylSunPhos-Daipen 双功能催化体系的存在下被氢化，对映过量高达 99.5%。在苯环上引入一个易于去除的邻溴原子后，通过氢化方法得到了对映体富集的 4-氯苯基吡啶甲醇，ee 值为 97.3%，这为一些组胺 H(1)拮抗剂提供了一个重要的手性中间体。
