Recent Progress in Metal‐Mediated and Catalyst‐Free Methods for Diarylureas Formation

ABSTRACT Diarylurea derivatives are cornerstone of organic chemistry, playing critical role in pharmaceuticals, agrochemicals, and materials science. Their biological relevance is well established and includes their presence in kinase inhibitors such as sorafenib, as well as in diuretics, antivirals, and a range of agrochemicals, including herbicides and pesticides. These compounds interact effectively with biological targets due to their hydrogen‐bonding capabilities and metabolic stability. At the molecular level, the electrophilic carbonyl and resonance‐active nitrogen atoms render ureas both reactive and stable. Their use as bioisosteres of amides or carbamates enhances pharmacokinetics and binding selectivity in medicinal chemistry. Advances in synthetic methodologies from traditional palladium or copper‐catalyzed reactions to greener strategies such as CO 2 fixation, metal‐free isocyanide insertions, and recyclable metal oxalates have made urea synthesis more sustainable and scalable.