A Cu‐(II) catalyzed N‐formylation and N‐acylation of amines with moderate to excellent yields, using N, N‐dimethyl formamide (DMF) and N, N‐dimethyl acetamide (DMA) as a formyl and acylating sources in the presence of 1,2,4‐triazole is reported. This novel, highly efficient and simple protocol shows broad substrate scope for aliphatic, aromatic, and heterocyclic amines. In addition, the conditions to prevent N‐formylation and N‐acylation impurities in the C−N cross coupling of amines and aryl halides are described typically when DMF and DMA are used as solvents, with various catalysts, ligands, and bases.
The Pd-II catalysed CÀ C bond formation Heck and Suzuki coupling reactions with moderate to excellent yields are reported, using curcumin as ligand, which is extracted from turmeric powder. The application of curcumin based [Pd(Curc-H) 2 ] catalyst in organic synthesis tested here, is the novelty of this protocol. This novel, highly efficient and simple protocol shows a broad substrate scope for aryl halides, substituted alkenes and phenyl boronic acid as coupling partners.
A simple and efficient protocol of Ni‐(II) catalyzed C−C bond formation in Heck coupling reactions of a variety of alkenes and aryl and hetero aryl halides, using various N‐aryl ethanolamines as bi‐dentate N,O‐ligand with moderate to excellent yields is described here. The application of different N‐aryl ethanolamines in presence of NiCl2.6H2O catalyst is tested for C−C bond formation in Heck reactions and found to be efficient in homogeneous medium. This simple and efficient protocol shows a broad substrate scope for substituted alkenes, aryl and hetero aryl halides and tolerates various functional groups and successfully demonstrated by 31 examples.
The presented study explores the anticancer potency of a novel series of chalcone clubbed 2,4‐dimethyl‐1H‐pyrrole‐3‐carboxamide derivatives. In vitro antimicrobial screening concluded that five compounds are potential against Candida albicans having inhibition of growth in the range of 46.38%–73.05% against at the concentration of 32 μg/mL. The antiproliferative screening against 60 cancer cell lines revealed that seven compounds have great potential against the various types of cancer cell lines with inhibition of growth in the range of 41%–71%. The structure–activity relationship study concluded that the hydrazide bond is more significant than the carboxamide bond. In silico study of highly potential derivatives obeys each parameter of Lipinski rule of five and qualified drug‐likeness behavior. The presented pyrrole‐chalcone template delivered various candidates as anticancer agents, and those could be a potential scaffold to develop the new anticancer drug.
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