Journal ArticleDOI
"Multi-component reactions : emerging chemistry in drug discovery" 'from xylocain to crixivan'.
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TLDR
This review details developments of new, highly atom-economic MCR derived chemical methods, which enable the fast and efficient production of chemical libraries comprised of a variety of biologically relevant templates, and focuses on applications of isocyanide based MCR (IMCR) reactions.Abstract:
With the recent emergence of combinatorial chemistry and high-speed parallel synthesis for drug discovery applications, the multi-component reaction (MCR) has seen a resurgence of interest. Easily automated one-pot reactions, such as the Ugi and Passerini reactions, are powerful tools for producing diverse arrays of compounds, often in one step and high yield. Despite this synthetic potential, the Ugi reaction is limited by producing products that are flexible and peptide-like, often being classified as 'non drug-like'. This review details developments of new, highly atom-economic MCR derived chemical methods, which enable the fast and efficient production of chemical libraries comprised of a variety of biologically relevant templates. Representative examples will also be given demonstrating the successful impact of MCR combinatorial methods at different stages of the lead discovery, lead optimization and pre-clinical process development arenas. This will include applications spanning biological tools, natural products and natural product-like diversity, traditional small molecule and 'biotech' therapeutics respectively. In particular, this review will focus on applications of isocyanide based MCR (IMCR) reactions.read more
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An Effective and New Method for the Synthesis of Polysubstituted Imidazoles by the Use of CrCl3.6H2O as a Green and Reusable Catalyst: Synthasis of Some Novel Imidazole Derivatives
TL;DR: In this paper, a new, efficient and environmentally adapted synthesis of polysubstituted imidazoles in one-pot is found, where the multicomponent reaction of various aldehydes, benzil, aliphatic and aromatic primary amines and ammonium acetate under solvent-free condition is explained.
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Rapid generation of molecular complexity using “hybrid” multi-component reactions (MCRs): application to the synthesis of α-amino nitriles and 1,2-diamines
TL;DR: Methyleneaziridines can be converted into a wide range of 1,2-diamines and 2-cyanopiperidines in a single operation with the formation of three intermolecular carbon-carbon bonds using a "hybrid" MCR.
Journal ArticleDOI
An efficient, multicomponent, green protocol to access 4, 7-dihydrotetrazolo [1, 5-a] pyrimidines and 5,6,7,9-tetrahydrotetrazolo[5,1-b]quinazolin-8(4H)-ones using PEG-400 under microwave irradiation
Shaik Firoj Basha,Tangella Nagendra Prasad,Veera Babu Gudise,Vadiga Shanthi Kumar,Naveen Mulakayala,Shaik Anwar +5 more
TL;DR: In this article, a facile one-pot synthesis of 5-aminotetrazole and diketones was described via a three-component reaction of aldehyde, 5-AMT, and 5-amT under microwave irradiation at 110'°C for 30'min.
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Recent advances and prospects in the Zn-catalysed Mannich reaction
TL;DR: A review of the recent advancements in the Zn-catalysed Mannich reaction, covering the literature from 2011 to 2020, can be found in this paper, where the authors summarise the most recent advancements.
Journal ArticleDOI
Synthesis of peptidomimetics, δ- And ε-lactam tetrazoles
TL;DR: A concise two-step procedure for the synthesis of novel δ-lactam tetrazoles has been established via the Ugi-azide reaction using 5-oxohexanoic acid along with primary amines, isocyanides, and azidotrimethylsilane followed by 1,1′-carbonyldiimidazole-mediated intramolecular amide formation.