Diastereoselective arylation of enantiopure 3-bromopiperidin-2-one derived from (R)-(−)-2-phenylglycinol with organocuprate reagents

The diastereoselective substitution of 3-bromolactam derived from (R)-(−)-2-phenylglycinol with a variety of arylcuprate reagents is presented. The stereochemical outcome of the substitution reaction is discussed. The method provides an efficient and straightforward route to enantiopure 3-arylpiperidines.