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

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 enantioselec...

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Bibliographic Details
Published in:Organic letters 2016-07, Vol.18 (13), p.3082-3085
Main Authors: Huang, Wen-Xue, Liu, Lian-Jin, Wu, Bo, Feng, Guang-Shou, Wang, Baomin, Zhou, Yong-Gui
Format: Article
Language:English
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Summary: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.6b01190