The preparation of optically active lactams from 3‐aryl‐2‐piperidinone is reported. The quaternary carbon stereocentres were formed using palladium‐catalysed asymmetric allylic alkylation reactions. The resulting enantioenriched compounds are useful intermediates for the synthesis and development of neurokinin antagonists.
A very simple method for obtaining a-arylated N-benzyl-2-piperidinones in high yields is described. The use of s-BuLi as the base and Pd(dba) 2 as the catalyst are the key factors.
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