A Simple Method of Synthesis of (±)-2,3-Diarylpiperazines and a Novel Method of Resolution of (±)-2,3-Diphenylpiperazine
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Intramolecular reductive coupling of diimines in the presence of Zn/Ti(OiPr)2Cl2 gives the corresponding (±)-2,3-diarylpiperazines in 73−83% yields with dl/meso ratio >99%:<1%. The (±)-2,3-diphenylpiperazine obtained in this way was readily resolved partially using l-(+)-tartaric acid, and the enantiomeric purity was enhanced to >99% ee via preparation of hydrogen-bonded salt aggregates using oxalic acid.
创建时间:
2016-05-05



