The first example of a retro-Henry type reaction is reported using 3-hydroxy-3-((3-methyl-4-nitroisoxazol-5-yl)methyl)indolin-2-ones which are prepared via catalyst-free Henry reaction of 3,5-dimethyl-4-nitroisoxazole and isatin.

A simple, metal-free protocol is reported for the one-pot synthesis of 2-styrylquinolines using a combination of 1,3-dimethyl urea (1,3-DMU) and L-tartaric acid (LTA) (in 3:1 ratio) as deep eutectic solvent...

Objective: Synthesis of novel 2-(1-benzofuran-2-yl)-N'-[(3Z)-2-oxo-1, 2-dihydro-3H-indol-3-ylidene] quinoline-4-carbohydrazide and its derivatives for antimicrobial and antitubercular activity.Methods: Synthesis was carried out using the general method and the structures were confirmed by IR, 1 Results:The results revealed that at 25 mg/ml concentration, compounds 3a and 5a showed good antibacterial activity at 3.5±0.1, 3.8±0.3, 3.6±0.2 respectively against E. coli, K. pneumonia and S. typhimurium, when compared with drug streptomycin with similar concentration. The percentage of inhibition found at 50 µg/ml concentration, compounds 2b and 6a exhibited good antifungal activity at 53±1.15, 57±1.52 against A. flavus and C. neoformans, compared with standard drug fluconazole. The increase in activity was found to be dose dependent. The analogue 2a showed good antitubercular activity at 12.5±0.5 µg/ml, compounds 2b, 3a, 4a-b, 5a-b and 6a-b exhibited significant activity at 25±0.57 µg/ml and compound 3b showed moderate activity at 50±0.57 µg/ml. The mean value of P<0.05 were considered to be statistically significant. The absorption, distribution, metabolism, excretion and toxicity studies of the entitled molecules were analyzed and found to be in acceptable range.H-NMR, [13]C-NMR and mass spectral analysis. The antibacterial activity was carried by agar well diffusion method, antifungal activity was performed by poison food technique and antitubercular activity was carried out by Microplate Alamar Blue Assay (MABA) method with the help of H37Rv. In silico absorption, distribution, metabolism, excretion, toxicity (ADMET) study of the drug, likeliness was carried out in ACD/lab-2. Conclusion:The study reveals that compounds containing benzofuran coupled nitrogen heterocycles are essential for activity as they possess excellent drug-like characteristics, suggesting to be potentially best inhibitor of H37Rv strain. The in silico ADME analysis also revealed that all the compounds were in acceptable range to obey the pharmacokinetic parameters.

Various isoxazole–oxindole hybrids were synthesized via vinylogous Henry reaction of 3,5-dimethyl-4-nitroisoxazole and isatin under catalyst free conditions in water. The products obtained were functionalized using 1,6-Michael addition reaction.

Catalyst-free synthesis of the isoxazole-spirooxindole-tetrahydrothiophene hybrids is reported. Formation of 1,4-thia-Michael and intramolecular aldol reactions were observed (instead of 1,6-thia-Michael followed by vinylogous Henry reactions) in a regioselective fashion to give new isoxazolespirooxindole-tetrahydrothiophene hybrids with excellent yields.

One-pot synthesis of isoxazole–thiolane hybrids are reported via the Knoevenagel condensation, domino sulfa-1,6-Michael/intramolecular vinylogous Henry reactions using piperidine (30 mol%) with >95% yields in 2–2.5 h overall reaction time.

Synthesis of 2-styryl-quinazolines and 3-styryl-quinoxaline based sulfonates is reported via sp3 C-H functionalization in the presence of triethylamine (10 mol%). The resulting compounds were tested for the α-glucosidase enzyme inhibition...

Correction for 'One-pot synthesis of functionalized isoxazole–thiolane hybrids via Knoevenagel condensation and domino sulfa-1,6-Michael/intramolecular vinylogous Henry reactions' by Sakkani Nagaraju et al., RSC Adv., 2015, 5, 94474–94478.