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Synthesis of Chiral Piperazines via Hydrogenation of Pyrazines Activated by Alkyl Halides

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Indexed by:期刊论文

Date of Publication:2016-07-01

Journal:ORGANIC LETTERS

Included Journals:SCIE、PubMed

Volume:18

Issue:13

Page Number:3082-3085

ISSN No.:1523-7060

Abstract:A facile method has been developed for the synthesis of chiral piperazines through Ir-catalyzed hydrogenation of pyrazines activated by alkyl halides, giving a wide range of chiral piperazines including 3-substituted as well as 2,3- and 3,5-disubstituted ones with up to 96% ee. The high enantioselectivity, easy scalability, and concise drug synthesis demonstrate the practical utility.

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