A series of pyrrole–2–carboxamide derivatives (4a–j) were synthesized and evaluated for theirantibacterial activity. Among the tested compounds, the most effective were 4a, 4b, 4c, 4d, 4e, 4g and 4h with MIC value in the range of 1.05–12.01 μg/mL against Gram–positive and Gramnegativebacterial strains. Further, the synthesized compounds have been screened for their invitro antifungal activity. In the present study, design and expeditious synthesis of novel 1–(4–chlorobenzyl)–N–(4–methoxybenzyl)–1H–pyrrole–2–carboxamide hybrid molecules as promising antibacterial agents.
A novel bicyclization strategy has been developed for the stereoselective synthesis of bicyclic lactones, i.e. 7-aryl or alkyl-2,6-dioxabicyclo[3.3.1]nonan-3-ones through a domino cyclization of (R)-3-hydroxyhex-5-enoic acid with an aldehyde in the presence of 10 mol% trimethylsilyltriflate under mild conditions. The salient features of this methodology are high yields, excellent selectivity, low catalyst loading and faster reaction times. This method has been successfully applied to the total synthesis of pyranopyran, tetraketide and polyrhacitide A.
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