3 years ago

Enantioselective Direct Synthesis of Free Cyclic Amines via Intramolecular Reductive Amination

Enantioselective Direct Synthesis of Free Cyclic Amines via Intramolecular Reductive Amination
Ying Zhang, Qiaozhi Yan, Guohua Hou, Guofu Zi
Chiral cyclic amines can be prepared via intramolecular reductive amination of N-Boc-protected amino ketones in a one-pot process. With the complex of iridium and f-spiroPhos as the catalyst, a range of N-Boc-protected amino ketones are smoothly transformed into chiral cyclic free amines in high yields and excellent enantioselectivities (up to 97% ee). Moreover, this method can also be successfully applied to the synthesis of a κ-opioid receptor selective antagonist, (S)-1.

Publisher URL: http://dx.doi.org/10.1021/acs.orglett.7b01828

DOI: 10.1021/acs.orglett.7b01828

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