Asymmetric hydrogenation for the synthesis of 2-substituted chiral morpholines |
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| Authors: | Mingxu Li Jian Zhang Yashi Zou Fengfan Zhou Zhenfeng Zhang Wanbin Zhang |
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| Institution: | Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240 China.; Frontier Science Center for Transformative Molecules, School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240 China |
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| 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.2-Substituted chiral morpholines were synthesized via a newly developed asymmetric hydrogenation of dehydromorpholines catalyzed by a bisphosphine–rhodium complex bearing a large bite angle. |
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