化学
动力学分辨率
立体中心
转移加氢
催化作用
对映选择合成
立体化学
有机化学
组合化学
钌
作者
Fangyuan Wang,Tilong Yang,Ting Wu,Long‐Sheng Zheng,Congcong Yin,Yongjie Shi,Xiang-Yu Ye,Genqiang Chen,Xumu Zhang
摘要
A catalytic protocol for the enantio- and diastereoselective reduction of α-substituted-β-keto carbonitriles is described. The reaction involves a DKR-ATH process with the simultaneous construction of β-hydroxy carbonitrile scaffolds with two contiguous stereogenic centers. A wide range of α-substituted-β-keto carbonitriles were obtained in high yields (94%–98%) and excellent enantio- and diastereoselectivities (up to >99% ee, up to >99:1 dr). The origin of the diastereoselectivity was also rationalized by DFT calculations. Furthermore, this methodology offers rapid access to the pharmaceutical intermediates of Ipenoxazone and Tapentadol.
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