Special Issue "Multicomponent Reaction"

Guest Editor
Dr. Irini Akritopoulou-Zanze
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-3500, USA
E-Mail:
Interests: drug discovery; de novo design and synthesis of biologically active scaffolds; focused compound libraries; multicomponent reactions

Dear Colleagues,

Multicomponent reactions (MCRs) are powerful transformations that incorporate portions of three or more reactants into new products in one pot procedures. They have been used extensively to form heterocyclic structures and they have been combined with subsequent transformations to yield complex structures, not easily accessible via classical synthetic reactions.
Efforts to discover new MCRs or further develop older ones, especially in combination with other transformations, contribute significantly to the advancement of organic synthesis by providing greater flexibility, novelty and efficiency. Applications of MCRs in drug discovery, material sciences, natural product synthesis and ligand and biological probe preparations further demonstrate the power of these reactions. Advances in cheminformatic tools allow for virtual MCR libraries to be first accessed in silico against a variety of different parameters before initiation of compound library synthesis.

This special issue of Molecules welcomes previously unpublished manuscripts covering all aspects of multicomponent reactions including their design, product assessment, methodology development and applications.

Dr. Irini Akritopoulou-Zanze
Guest Editor

Submission

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. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as 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 refereed through a 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 monthly 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 1400 CHF (Swiss Francs).

• multicomponent reactions
• isocyanide-based MCRS
• heterocycle forming MCRS
• library design
• library synthesis
• parallel synthesis
• novel scaffolds
• biologically active molecules
• post MCR transformations
• macromolecules

Type of Paper: Article
Title: Synthetic Studies of DMAP Derivatives by Diastereoselective Ugi Reaction
Authors: Hiroki Mandai, Irie Shunsuke, Koichi Mitsudo and Seiji Suga
Affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University;
E-Mail: mandai@cc.okayama-u.ac.jp (H.M.)
Abstract: Diastereoselective Ugi reactions of DMAP-based aldehydes with alpha-amino acids and tert-butyl isocyanide were examined. Reactions of 4-(dimethylamino)-2-pyridinecarboxaldehyde with various alpha-amino acids afford 2-substituted DMAP with low diastereoselectivities. Whereas, reactions with 4-(dimethylamino)-3-pyridinecarboxaldehyde deliver 3-substituted DMAP with moderate to high diastereoselectivities. The combination of alpha-amino acid and DMAP-based aldehyde are important to achieve high diastereoselectivity. The kinetic resolutions of secondary alcohols using thus obtained chiral DMAP were also examined.

Type of Paper: Article
Title: Divergent Synthesis of Novel Five-Member Heterocyclic Compounds by Base-Mediated Rearrangement of Acrylamides Derived from a Novel Isocyanide-Based Multicomponent Reaction
Authors: Andrea Basso, Luca Banfi and Renata Riva
Affiliation: Dipartimento di Chimica e Chimica Industriale, Università degli Studi di Genova, Italy; E-Mail: andrea.basso@unige.it (A.B.)
Abstract: We have recently reported a novel multicomponent reaction between arylacetic acids and isocyanides, affording alpha-acyloxyacrylamides through an unusual mechanism. We now wish to report that the products of this novel multicomponent reaction can rearrange to five member heterocyclic compounds when exposed to basic environment. Depending on the reaction conditions and on the substitution pattern on the substrates, various pyrrolidine derivatives can be selectively obtained. Phenotypic biological assays have shown interesting properties of some representative compounds.