Bioactive chemical space exploration via greener GBB multicomponent reaction

Multicomponent reactions (MCRs) are a green strategy in which a collection of molecules with great diversity is generated with minimum synthetic effort, time and by-products formation. Among the MCRs, the Groebke-Blackburn-Bienaymé (GBB) reaction have been used widely in medicinal chemistry. In particular, privileged structures of the imidazoheterocyclic type, which are ubiquitous structural motifs in bioactive molecules with interesting biological properties, can be efficiently obtained through the GBB reaction. 1-3

Continuing with our efforts to synthetize bioactive molecules via ecofriendly and sustainable MCRs, we studied the GBB reaction under green conditions. In the present work, this multicomponent reaction was optimized to achieve a set of products under the green chemistry guidelines in shortened reaction times using Monowave 50® assistance.4,5 Different aldehydes, amidines and isocyanides component were employed and combined. Consequently, a small library of compounds was prepared and evaluated for anti-helmintic and antiproliferative activity.