Green Methodologies for the Synthesis of Active Pharmaceutical Ingredients and Drug-Like Compounds

Dear Colleagues,

The identification of new drugs and pharmaceutical ingredients is a long, expensive, and time-consuming process, which every year leads pharmaceutical companies to spend billions of euros/dollars. On the other hand, the successful identification and marketing of new pharmaceuticals have high rewards, not only in terms of economic gain but most of all as immeasurable benefits to healthcare and to society. However, the synthetic processes to access active pharmaceutical ingredients (APIs), especially those developed in academia, are often unappealing at industrial level due to the use of stoichiometric rather than catalytic quantities of reagents, the use of protecting group strategies to ensure chemical selectivity, the consumption of large amounts of organic solvents to facilitate the synthetic processing, as well the requirement of prolonged heating times and the formation of potentially harmful reactive intermediates. Pharmaceutical industries have high interest in the identification of new strategic research to underpin the development of innovative and sustainable manufacturing routes to prepare high-value chemicals and drugs.

Medicinal chemistry has changed a lot in recent decades. At present, in addition to the design and identification of novel APIs, a modern medicinal chemist should take into account, during the synthesis of a drug, key aspects like the greenness, scalability, and, more in general, sustainability of a synthetic process. Methodologies which offer “greener” synthetic alternatives, such as the use of enzymes, light, organocatalysts, benign solvents, milder reaction conditions or multicomponent strategies to avoid the isolation of intermediates will offer significant improvements in the manufacturing and development of the medicines of the 21st century. Pharmaceutical companies are committed to finding novel ways to produce APIs with a minimum impact on the environment and high efficiency at once.

Within this context, this Special Issue wants to focus on the development of “Green Methodologies for the Synthesis of Active Pharmaceutical Ingredients and Drug-Like Compounds”. The aim of this issue is to present the advances in the field of green chemistry and technologies applied to the synthesis and manufacturing of drugs and APIs. In detail, the topics covered will be: (1) green approaches to the synthesis of drug-like compounds, synthons, and APIs; (2) catalytic methods (bio-, photo-, electro-, metal-catalyzed methods) in the synthesis of drugs; (3) chemical reactions in benign solvents for the synthesis of drugs (i.e., ionic liquids, deep eutectic solvents); and (4) flow, multicomponent, and combinatorial processes which avoid the isolation of synthetic intermediates.

Dr. Daniele Castagnolo
Guest Editor

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• Green chemistry
• Biocatalysis
• Photocatalysis
• Electrocatalysis
• Homogeneous and heterogeneous catalysis
• Flow chemistry
• Benign solvents
• Deep eutectic solvents
• Ionic liquids
• Multicomponent reaction
• Combinatorial chemistry
• Microwave-accelerated synthesis
• Drug synthesis
• Sustainable chemistry
• Atom economy