Journal
ORGANIC LETTERS
Volume 19, Issue 16, Pages 4215-4218Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b01828
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Funding
- National Natural Science Foundation of China [21672024, 21272026, 21472013]
- Beijing Municipal Commission of Education
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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 K-opioid receptor selective antagonist, (S)-1.
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