No abstract

For obtaining novel bioactive compounds with significant antifungal activities, a series of novel paeonol derivatives linked with a 1,2,3-triazole moiety have been designed and synthesised by a click reaction under mild conditions using Cu(OAc) 2 ·H 2 O/sodium ascorbate as a catalyst. The antifungal activities of all the target compounds were evaluated in vitro against two plant pathogenic fungi, Colletotrichum capsici and Rhizoctonia cerealis. Preliminary results indicated that 1-(4-methoxy-2-{[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl]-methoxy}phenyl)ethanone showed the best antifungal activities against C. capsici, while 1-(2-{[1-(2-fluorophenyl)-1H-1,2,3-triazol-4-yl]methoxy}-4-methoxyphenyl)ethanone and 1-(4-methoxy-2-{[1-(o-tolyl)-1H-1,2,3-triazol-4yl]methoxy}phenyl)ethanone were found to have better antifungal activities against the tested two fungi. All the synthesised compounds have been determined by IR, HR MS and NMR spectra.Scheme 1 Synthetic routes of the title compounds. Reagents and conditions: (a) NaOH, acetone, reflux, 48h, 23%; (b) Cu(OAc) 2 ·H 2 O(10 mol%), sodium ascorbate (20 mol%), t-BuOH/H 2 O (1:1), ultrasound irradiation, 30 °C. O O

Cu2O/CMP has been developed as a highly efficient catalytic system for Huisgen-click reaction in water at 60 °C.

An efficient and green protocol for the reduction of nitroaromatic compounds to the corresponding amines has been developed. The reduction catalyst system includes NH2NH2·H2O and H2O2-treated activated carbon. Without adding additional metals, the H2O2-treated activated carbon could be reused for many cycles without decreasing catalytic efficiency. The aromatic amines could be obtained in good to excellent yields.

In order to obtain novel bioactive compounds with significant antifungal activities, a series of 2H-1,4-benzoxazin-3(4H)-one analogs linked with a 1,2,3-triazole moiety have been designed and synthesized via click reactions in a one-pot process at room temperature using CuCl as the catalyst. Their antifungal activities were tested against two plant-pathogenic fungi, Rhizoctonia cerealis (RC) and Colletotrichum capsici (CC). Statistical analysis showed that among the tested compounds in particular compound 3a exhibits a significant growth inhibitory activity against both RC and CC. All the synthesized compounds have been characterized by IR, HRMS and NMR experiments.