Single-Step Synthesis of 5,6,7,8-Tetrahydroindolizines via Annulation of 2-Formylpiperidine and 1,3-Dicarbonyl Compounds.

ABSTRACT

An expedient single-step synthesis of 5,6,7,8-tetrahydroindolizines has been achieved via the annulation of commercially available 2-formylpiperidine hydrochloride and 1,3-dicarbonyl compounds in THF in the presence of pyrrolidine and 4 Å molecular sieves. A variety of ß-ketoesters, ketones, and amides participated in this annulation chemistry, affording the desired 5,6,7,8-tetrahydroindolizines in moderate to good yields.