Multicomponent reactions (MCR) in medicinal chemistry: a patent review (2010-2020)

Design, synthesis and biological evaluation of 1,5-disubstituted α-amino tetrazole derivatives as non-covalent inflammasome-caspase-1 complex inhibitors with potential application against immune and inflammatory disorders

“…Thus, we aimed to design non cleavable aspartyl mimicking scaffolds which would allow for easy modification in further positions to address P2–P4 sites. Multicomponent reaction chemistry is known to address a large drug-like scaffold space and is compatible to multiple functional (often unprotected) groups [ [41] , [42] , [43] ]. For example, MCR has been recently used for the improved synthesis of the drugs atorvastatin, praziquantel and ivosidenib [ [44] , [45] , [46] ].…”

The evaluation of chemoselectivity in multicomponent domino Knoevenagel/Diels-Alder reaction: A DFT study

“…6 By the way, the development of domino and other multicomponent reaction methodologies can provide convenient admission to produce more complex compounds from simple starting materials. 2,7,8 The incorporation of a Diels-Alder reaction sequence is the fundamental key to many interesting variants of these reactions. [9][10][11] In recent times, organocatalysis has emerged as a promising synthetic tool for constructing C-C and C-N bonds in aldol, 12 Michael, 13 Mannich, 14 Diels-Alder 15 and other reactions 16 with very good chemoelectivity and stereoselectivity.…”

Fluorene-Based Multicomponent Reactions

“…It gives access to huge libraries due to its four points of diversification, and it also serves as an excellent hub for a plethora of secondary transformations. 51,52 We employed both the isocyanide 1 and the fluorene-based aldehyde and amine to obtain the corresponding bisamides 5a-c in yields of 34-89%, respectively. Notably, in the case of 5c, three molecules of fluorene were incorporated into one adduct, demonstrating a favorable architectural aspect of this reaction (Figure 2).…”