Li Mingxu, Zhang Jian, Zou Yashi, Zhou Fengfan, Zhang Zhenfeng, Zhang Wanbin
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.
Chem Sci. 2021 Oct 28;12(45):15061-15066. doi: 10.1039/d1sc04288b. eCollection 2021 Nov 24.
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.
通过使用具有大咬合角的双膦 - 铑催化剂，已开发出不饱和吗啉的不对称氢化反应。采用这种方法，可以以定量产率和优异的对映选择性（高达99% ee）获得多种2 - 取代的手性吗啉。氢化产物可转化为生物活性化合物的关键中间体。
