No abstract

An efficient and green copper(II) acetylacetonate-catalyzed protocol for the Huisgen-click reaction in water at 100 ℃ has been established. The protocol was not only suitable for the reaction between organic azides and alkynes, but also suitable for one-pot three-component reaction among alkyl halides, NaN 3 and alkynes.

A convenient CuI/DBU catalyzed one-pot method has been developed for the synthesis of 1,4-disubstituted 1,2,3-triazoles from aryl iodides, sodium azide and phenylacetaldehyde derivatives or from aryl iodides, sodium azide and alkynes in DMSO.

For finding novel bioactive compounds with significant antifungal activities, 17 novel benzoxazole derivatives containing a 1,2,3-triazole moiety were synthesized by the copper(II) acetylacetonatecatalyzed cyclization reaction between 2-aminophenol derivatives and 1H-1,2,3-triazole-4carbaldehyde derivatives (4a), which were prepared through three steps using aromatic amine as the starting material. Antifungal activities of the prepared compounds were evaluated against Botrytis cinerea (BC) and Fusarium Verticillium (FV). The test results indicated that compounds 5b, 5c, 5h, and 5n show good inhibitory effects on fungi. The preliminary structure-activity relationship is also discussed.