Asymmetric hydrogenation for the synthesis of 2-substituted chiral morpholines

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.

PMID:34909146 | PMC:PMC8612400 | DOI:10.1039/d1sc04288b


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