The pyrrolidine fragment is a privileged scaffold within chiral ligands employed in coordination complexes exhibiting catalytic activity in asymmetric reactions and, more recently, as enantioselective organocatalysts per se. Likewise, the employment of (S)-proline as starting material constitutes the most direct form to synthesize those chiral derivatives. Afterwards, a preliminary evaluation of the catalytic performance of proline-derived compounds consists of screening many prochiral substrates in well standardized model reactions such as Michael additions and Mannich reactions, with the aim of identifying “broad spectrum” catalysts for more complex synthetic applications. Therefore, a central part of this process involves the fast and direct measurement of enantioselectivities of optically active adducts. The growing development of chiral stationary phases and thus, the wide commercial availability of chiral columns have consolidated high performance liquid chromatography (HPLC) as the preferred technique to identify the most effective catalysts.

The use of microwave heating is a valuable tool for synthetic chemists. Being able to reduce reaction times and to increase product yield, this methodology offers to organic chemists the potential to optimize reaction processes. Additionally, microwave-assisted reactions provide more environmentally friendly reaction conditions. In this report, we describe results in the optimization of several organic reactions employed in the synthesis of various chiral molecules such as heterocycles, β-amino acids, and β-peptides, among others.

El uso de calentamiento por microondas es una valiosa herramienta para los químicos sintéticos. Esta metodología permite reducir los tiempos de reacción e incrementar el rendimiento de los productos, lo que equivale a optimizar los procesos de interés. Aunado a esto, las reacciones asistidas por microondas son más amigables al medio ambiente. En este trabajo se describen algunos resultados obtenidos en la optimización de varias reacciones orgánicas utilizadas para la síntesis de diversas moléculas quirales tales como heterociclos, β-aminoácidos y β-péptidos, entre otros.