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Catalytic Asymmetric Synthesis of Substituted Morpholines and Piperazines


  • The authors gratefully thank Zalicus Pharmaceuticals Ltd for biological screening assays and NSERC for financial support of this work. The authors thank Dr. Brian O. Patrick for assistance with X-ray crystallography.


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Under two conditions: Hydroamination catalyzed by group 4 metals is featured in the modular and enantioselective synthesis of 3-substituted morpholines and the diastereoselective synthesis of 2,5-substituted piperazines.