Organic Communications Articles

The polymer supported carvacrol anion was reacted with 1,2-dibromoethane, 1,4-dibromoethane, oxalyl dichloride, malonyl dichloride, succinyl dichloride, glutaroyl dichloride, and adipoyl dichloride to afford the corresponding dimeric carvacryl ethers or esters.

A variety of β-acetamido ketones and ketoesters are readily prepared in high yields under extremely mild conditions via a three component coupling of aromatic aldehydes, enolizable ketones or β-ketoesters and nitriles in the presence of 10 mol% of copper(II) tetrafluoroborate and a stoichiometric amount of acetyl chloride. A solution of 10 mol% of Cu(BF 4) 2 in acetonitrile provides a convenient reaction medium to carry out a three component reaction under mild conditions

A series of novel methylene-bis-[1,5]-benzothiazepines 4 andmethylene-bis-benzofuranyl-[1,5]-benzothiazepines 5 were prepared by the reaction of methylene-bis-chalcones 3 with 2-aminothiophenol followed by the condensation with α-bromoacetophenone. The structures of the synthesized compounds were confirmed by their IR, 1H, 13C NMR and Mass spectral analyses. All the synthesized compounds were tested for their antimicrobial activity against Gram-positive, Gram-negative bacteria and fungi. Among the synthesized compounds, the compounds 4f, 4g, 5f and 5g were found to be the most active against Bacillus subtilis, Bacillus sphaericus, Staphylococcus aureus, Klebsiella aerogenes and Chromobacterium violaceum. Similarly these compounds showed potent antifungal effect against Candida albicans, Aspergillus fumigatus, Trichophyton rubrum, and Trichophyton mentagrophytes. It is interesting to note that the compounds with heterocyclic ring substituents at the 4th position of benzothiazepine system displayed notable antibacterial activity, almost equal to that of streptomycin and penicillin.