Organocatalysis: Past, Present, and Future Perspectives

Dear Colleagues,

Since the seminal work of the 2021 Nobel Prize Winners for Chemistry, Professors David W. C. MacMillan and Benjamin List, in the late 1990s, organocatalysis has recorded an extraordinary blossoming to the point that it can now be counted as one fundamental pillar of (asymmetric) catalysis, paralleling and complementing to metal-catalyzed reactions and biocatalysis. In fact, the publication of about 1500 articles per year in the last decade is proof of the great growth of organocatalysis, which undoubtedly represents one of the fastest-growing themes in Chemistry.

The enormous interest of so many research groups in organocatalytic reactions stems from some typical distinguishing features, among which operational simplicity, tolerance to air and moisture, and, with specific reference to catalysts, high stability/robustness, non-toxicity, wide functional group tolerance, and broad molecular diversity, also made possible drawing on members of the “chiral pool” (e.g., alkaloids, amino acids, carbohydrates) or their derivatives.

Application fields of organocatalysis are innumerable, ranging from aminocatalysis, Brønsted-acid catalysis, H-bonding catalysis, N-heterocyclic carbene catalysis, ion-pairing catalysis, and oligopeptide (foldamers) catalysis to SOMO activation, organosuperbases/frustrated Lewis pairs promoted catalysis, bifunctional catalysis, and synergistic catalysis, among others. In addition, it should also be said that organocatalysis has been shown to be mature for one-pot and cascade/tandem reactions, total syntheses, and application in both polymer and medicinal/pharmaceutical chemistry.  

Importantly, organocatalysis has implications for the mission of green chemistry, so much so that, in 2019, IUPAC identified this technology as one of the 10 emerging ones in Chemistry with potential to achieve a more sustainable planet. Specific strategies can be adopted to serve this purpose, including intensification techniques (e.g., ball milling, flow, ultrasound, microwave, light, and high pressure), alternative reaction media (i.e., water, supercritical fluids, ionic liquids, deep eutectic solvents, and biomass-derived solvents), as well as solvent-free conditions. No less important is the possible catalyst immobilization, which can play in favour of catalyst recycling. This is a particularly important aspect in the case of high-cost catalysts, and is especially suitable for flow techniques and/or particular reaction media.

Surely, there might be room for further development, new trends in organocatalysis being expected through combination with some emerging technologies (electrochemistry, photocatalysis, and chemoinformatics). However, other than that, the adoption of catalysts derived from renewable biomass feedstocks could allow organocatalysis to consolidate its role for the benefit of circular economy and sustainability, while new frontiers could be set in chemical biology and biomedicine by developing promoters capable of operating in water and biological milieu.

Given all that, this Special Issue of Molecules is meant to collect original research articles and reviews on the topic of organocatalysis in all its possible applications.

Dr. Carmela De Risi
Guest Editor

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• organocatalysis
• asymmetric organocatalysis
• green organocatalysis
• aminocatalysis
• H-bonding catalysis
• N-heterocyclic carbene catalysis
• bifunctional catalysis
• synergistic catalysis
• photo-organocatalysis
• heterogeneous organocatalysis
• continuous-flow organocatalysis