Advances in microwave-assisted synthesis and the impact of novel drug discovery

Abstract

Microwave (MW)-assisted synthesis of biologically active compounds has received a lot of attention in the last decades due to the advantages that such a technique offers compared to traditional heating procedures. Areas covered: The authors provide a focused review on the recent applications of this technique for drug design purposes. MW syntheses have been used for designing libraries of compounds, in combinatorial and multicomponent approaches, for lead optimization, as well as for forcing reactions which do not occur or occur in low yields using traditional methods. Expert opinion: This technique offers significant advantages over the traditional heating due to the fact that the reaction time is shortened, the possibility to have concurrent side reactions is decreased and the use of smaller amounts of polluting solvents is also reduced. However, no significant technical advances have been reported for MW-assisted devices in the last years, with the important novelty being only in the type of reactions/compounds that have been investigated and synthesized using the MW heating approach.

A Perspective on Innovating the Chemistry Lab Bench

“…Automated solid-phase peptide synthesis, despite having initially developed well over 50 years ago (Merrifield, 1963), continues to experience advancements in its chemistry and functional versatility (Isidro-Llobet et al, 2019). Newer experimental techniques mediated through microwave irradiation (Berrino and Supuran, 2018), photo-redox catalysis (Shaw et al, 2016), and electrochemically mediated organic synthesis (Yan et al, 2018) continue to expand the synthetic chemist's toolbox expanding the options for more versatile engineered automation solutions. Continued additions to the chemistry methodology compendium will undoubtedly lead to an expansion of the scope of chemistry that will be inherently automatable and help reduce the need and the expense for more bespoke systems developed for transformations of much narrower scope.…”

Microwave assisted synthesis and antimicrobial evaluation of symmetrical 1,2-Phenylenediamine Schiff’s base derivatives

“…In addition, the technique is assumed as an significant application in the direction of green chemistry, since this technique is friendly to the environment. 16,17 Material and methods…”

Sustainable Synthesis of a Potent and Selective 5-HT7 Receptor Antagonist Using a Mechanochemical Approach

“…In the last decades, different techniques have been developed, for example, microwave-assisted organic chemistry and flow chemistry, which might reduce the time required to generate compound libraries for biological screening or might ensure more efficient production of active pharmaceutical ingredients (APIs). 1 − 4 Recently, mechanochemical synthesis has also been recognized as an innovative methodology, 5 with a wide range of practical applications in both academic and industrial research. In particular, mechanochemistry has been used to produce various families of compounds.…”

“…Synthetic organic chemistry represents a key component of many drug discovery programs. In the last decades, different techniques have been developed, for example, microwave-assisted organic chemistry and flow chemistry, which might reduce the time required to generate compound libraries for biological screening or might ensure more efficient production of active pharmaceutical ingredients (APIs). − Recently, mechanochemical synthesis has also been recognized as an innovative methodology, with a wide range of practical applications in both academic and industrial research. In particular, mechanochemistry has been used to produce various families of compounds. − The primary driving force underlying the rediscovery of mechanochemistry is green chemistry, − in particular, the need of chemical and pharmaceutical industries for the development of more sustainable synthetic protocols characterized by the energy efficiency of chemical transformations and reduction of solvent use.…”