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Synthesis and Chemoenzymatic Approaches to Pharmaceutically Relevant Products and Intermediates

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: 30 October 2026 | Viewed by 257

Editors

Department of Pharmaceutical Science, University of Milan, Milan, Italy
Interests: organic synthesis; structural characterization of molecules with biological interest; solid-state characterization of nanoparticle systems for drug delivery; analytical techniques (UV, NMR, FTIR, XRPD, DSC)

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Guest Editor
Department of Pharmaceutical Science, University of Milan, Milan, Italy
Interests: biocatalysis; chemoenzymatic reactions; organic synthesis

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Guest Editor
Department of Pharmaceutical Science, University of Milan, Milan, Italy
Interests: organometallic chemistry; catalysis; transition metal complexes; biological active molecules; asymmetric synthesis
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Special Issue Information

Dear Colleagues,

The discovery and development of efficient strategies for the preparation of pharmaceutically relevant products and intermediates remain central topics in medicinal chemistry. Accordingly, the exploration of new synthetic approaches for the production of advanced pharmaceutical intermediates has become an important research focus. Among these, innovative methods include metal-promoted reactions as well as biosynthetic and catalytic approaches.

Transition metal catalysis plays a crucial role in pharmaceutical synthesis, with noble metals such as Pd-, Ir- and Rh-based catalysts enabling highly selective and enantioselective transformations, including cross-coupling reactions, hydrogenations, and C–H activations. Conversely, earth-abundant metals (e.g., Fe, Cu, Zn) offer more sustainable and cost-effective alternatives. Together, these, metal catalysts provide a complementary toolkit for the synthesis of diverse heterocyclic frameworks, which form the core of countless bioactive compounds.

Traditional synthesis methods, however, still struggle to fully meet the demands for structural complexity and high purity for pharmaceutical intermediates. In this context, innovative chemoenzymatic and multicomponent strategies that combine enzymatic selectivity with the versatility of chemical synthesis represent an attractive alternative.

Over the past decade, such integrated approaches have increasingly exploited the strengths of both chemical catalysis and biocatalysis, enabling the selective and environmentally benign synthesis of pharmaceutical compounds. Nevertheless, further advances are required to improve catalyst compatibility, enzyme stability, and overall reaction efficiency.

Submissions of original articles and reviews focusing on the synthesis and spectroscopic characterization of biologically active compounds and intermediates—either via classical chemical synthesis or in combination with biotransformation reactions—are encouraged. Contributions addressing sustainable and innovative strategies in the design of pharmaceutical products and intermediates will further enrich this Special Issue.

Dr. Elena Pini
Prof. Raffaella Gandolfi
Dr. Giorgio Facchetti
Guest Editors

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 250 words) can be sent to the Editorial Office for assessment.

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-anonymized 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.

Keywords

  • organic synthesis
  • chemoenzymatic synthesis
  • active pharmaceutical ingredients (APIs)
  • pharmaceutical intermediates
  • drug development
  • organometallic catalysis
  • stereo-controlled reactions

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Published Papers

This special issue is now open for submission.
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