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Published on: November 9, 2019
Asymmetric hydrogenation for the synthesis of 2-substituted chiral morpholines
Mingxu Li1, Jian Zhang1, Yashi Zou1
1Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University 800 Dongchuan Road Shanghai 200240 China zhenfeng@sjtu.edu.cn.
Abstract:
Asymmetric hydrogenation of unsaturated morpholines has been developed by using a bisphosphine-rhodium catalyst bearing a large bite angle. With this approach, a variety of 2-substituted chiral morpholines could be obtained in quantitative yields and with excellent enantioselectivities (up to 99% ee). The hydrogenated products could be transformed into key intermediates for bioactive compounds.
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