Journal ArticleDOI
"Multi-component reactions : emerging chemistry in drug discovery" 'from xylocain to crixivan'.
Reads0
Chats0
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
Citations
More filters
Journal ArticleDOI
One-pot access to a library of structurally diverse nicotinamide derivatives via a three-component formal aza [3 + 3] cycloaddition.
TL;DR: The three-component formal [3 + 3] aza-annulation between chalcones, β-ketoamides, and ammonium acetate in the presence of CAN as a Lewis acid affords good to excellent yields of highly substituted nicotinamides or their fused derivatives.
Journal ArticleDOI
ZnO‐NR as the efficient catalyst for the synthesis of new thiazole and cyclopentadienone phosphonate derivatives in water
Zinatossadat Hossaini,Daryoush Zareyee,Fatemeh Sheikholeslami-Farahani,Samaneh Vaseghi,Afshin Zamani +4 more
Journal ArticleDOI
[Bmim]BF4: A Versatile Ionic Liquid for the Synthesis of Diverse Bioactive Heterocycles
Journal ArticleDOI
Boehmite nanoparticles, an efficient green catalyst for the multi-component synthesis of highly substituted imidazoles
TL;DR: Boehmite nanoparticles (AlOOH NPs) were found to be a highly active and green catalyst for the synthesis of highly substituted imidazoles under solvent-free conditions.