A simple and effective synthetic approach to chiral 4-pyridinyl proline derivatives

A rapid approach has been developed to provide a novel series of 4-pyridinyl proline derivatives as potential stereoselective catalysts. Nucleophilic displacement at the 4-pyridinyl position proved straightforward using proline but required microwave heating to proceed when using the more bulky α-methyl proline. Total control of enantioselectivity was obtained for the synthesis of proline derivatives.