2,5-diketopiperazines (2,5-DKPs) are the smallest cyclic peptides in nature and display a variety of antibacterial, antifungal, and anticancer properties. Very little has been reported on the one-pot synthesis of 2,5-DKPs. Herein, we report a novel one-pot synthesis of 2,5-DKPs via the Ugi-4CR/S_N2-cyclization strategy, under mild conditions, and ethanol was used as a solvent for both procedures.

2,5-DKPs are heterocyclic peptidomimetics, present in nature with high structural diversity, popular in the design of new bioactive molecules with potential application in medicinal chemistry, exhibiting anticancer and antimicrobial properties, among others. Therefore, in the present work, we report the one-pot synthesis of 2,5-DKPs and their links to another heterocycle 1,4-disubstituted 1,2,3-triazole under mild reaction conditions by one-pot process via the sequence IMCR/postransformation/CuAAC with several advantages over previously reported conventional methods.

The synthesis of Imidazo[1, 2-a]pyridine (IMP) analogs is a research field constantly growing due potential applications of Groebke–Blackburn–Bienaymé (GBB) products in several fields, focusing on the development of novel greener strategies. To date, the ultrasound assisted synthesis of IMP analogs via Groebke–Blackburn–Bienaymé reaction (GBBR) under green inexpensive catalysts such p-toluenesulfonic acid (TsOH) is practically unreported. In the present work, we describe the TsOH catalyzed GBB reaction assisted by ultrasound irradiation (USI) to access IMP analogs in excellent overall yields 77–91%.

Imidazo[1,2-a]pyridines (IMPs) are valuable heterocycles, present in bioactive compounds and drugs. Analogs that incorporate azide moieties are useful intermediates in organic synthesis and can be used as synthetic platforms to access more complex products. Isocyanide-based multicomponent reactions such as Groebke–Blackburn–Bienaymé (GBB-3CR) are versatile tools to synthesized IMPs, in which orthogonal reagents are included into components to increase its synthetic potential. Herein we developed a one-pot process to access IMPs functionalized with azides under mild conditions, which are synthetic platforms for further post-transformations.

Lipid droplets (LDs) and the endoplasmic reticulum (ER) are dynamic organelles central to cellular metabolism, signaling, and stress response. Despite their biological relevance and close interplay, tools to selectively track their dynamic behavior remain limited. Here, the design, synthesis, and characterization of a new class of fluorescent probes obtained through green multicomponent synthetic strategies are reported. These previously unexplored fluorophore scaffolds display unexpected and differential subcellular localization, selectively targeting either LDs or the ER with high photostability. Mechanistic studies suggest that such selectivity arises from a synergistic interplay between partition coefficient, conformational geometry, and strategically positioned targeting moieties. These features enable the probes to adapt to distinct microenvironments within cells, supporting real‐time visualization of both LD and ER dynamics. These findings provide versatile sensing tools and novel insights into organelle‐targeting principles, establishing an eco‐conscious route to next‐generation fluorescent sensors.

1,5-disubstituted tetrazoles (1,5-Ds-T) are heterocyclic bioisosteres of the cis-amide bond, commonly found in bioactive compounds, pharmaceuticals, and functional materials. Chromones are privileged scaffolds widely present in natural products that are well known for their diverse biological activities, including anticancer, antimicrobial, antidiabetic, anti-inflammatory, and antioxidant properties. Isocyanide-based multicomponent reactions, such as the Ugi-Azide (UA-4CR), provide a versatile strategy for synthesizing 1,5-Ds-T, which can be incorporated into other privileged heterocyclic or commercially available drugs. Herein, we describe a sonochemical one-pot synthesis of 1,5-Ds-T connected to chromone under mild conditions, highlighting their potential relevance in medicinal chemistry.