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

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.