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

作者: Wen-Xue Huang , Lian-Jin Liu , Bo Wu , Guang-Shou Feng , Baomin Wang

DOI: 10.1021/ACS.ORGLETT.6B01190

关键词: HalideOrganic chemistryAlkylDrug synthesisChemistry

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

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