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

✍ Scribed by Ghislaine Priem; Mike S. Anson; Simon J.F. Macdonald; Béatrice Pelotier; Ian B. Campbell

• Publisher: Elsevier Science
• Year: 2002
• Tongue: French
• Weight: 303 KB
• Volume: 43
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(02)01255-8

✦ Synopsis

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 a-methyl proline. Total control of enantioselectivity was obtained for the synthesis of proline derivatives.