The mixture of enantiomers in most cases leads to unfavorable outcomes in a biological organism. Historically, one of the most representative examples is thalidomide—an antiemetic drug synthesized and administered to pregnant women in its racemic form during the 1950s—where the R-enantiomer exhibited the desired effect, while the S-enantiomer showed teratogenic effects.

In this context, another group of drugs for which it is important to regulate the administration of only one enantiomer are non-steroidal anti-inflammatory drugs (NSAIDs). Some, like R-naproxen, are marketed in enantiomerically pure form, while others such as ibuprofen and ketoprofen, are sold as racemates.

Given that patients requiring this type of drug often take them for extended periods, research has focused on the chiral and efficient synthesis of only the active stereoisomer. Therefore, the present work describes the synthesis of a new chiral catalyst that features a palladium atom as the central metal and the dipeptide L-lysine-glycine as the ligand. The catalyst was characterized by electron microscopy, infrared spectroscopy, nuclear magnetic resonance, and mass spectrometry.

Its ability to induce chirality was tested in an aldol reaction between various aromatic aldehydes and cyclohexanone, achieving good yields and enantiomeric excesses of up to 75%, as determined by high-performance liquid chromatography. Additionally, due to the presence of a palladium metal center, it was evaluated in a Heck cross-coupling reaction, where it was observed to promote C–C bond formation. This suggests that the catalyst could potentially be used in one-pot processes involving aldol–Heck reactions.