N-烃氧羰基-2-噻唑烷酮衍生物的合成及其杀菌活性(英文)

Synthesis and Fungicidal Activities of N-Carboalkoxy(aryloxy)-2-thiazolidinones

为了寻求新的杀菌先导化合物,通过 2 噻唑烷酮与氯甲酸酯的缩合反应得到 11个N 烃氧羰基 2 噻唑烷酮衍生物(5a^5k),其中 10个为新化合物,其结构均经 1HNMR、MS、IR和元素分析表征。初步离体杀菌实验结果表明,大多数化合物较之母体 2 噻唑烷酮具有更高的杀菌活性。在浓度为 2 000 mg/L下,化合物 5c、5d、5e、5f、5g、5h、5i、5j对油菜菌核病菌Sclerotiniasclerotiorum的抑制率为 100%, 5i对番茄灰霉病菌Botrytiscinerea、柑桔青霉病菌Penicilliumitalicum和油菜菌核病菌的抑制率均为 100%。

In order to find new fungicidal lead compounds, eleven N-carboalkoxy(aryloxy)-2-(thiazolidinones,) ten of which are novel compounds, were prepared from a condensation reaction of (2-thiazolidinone) and chloroformate, and their structures were confirmed by ^(1)H NMR, MS, IR and (elemental) analysis. The results of fungicidal tests, at the concentration of 2 000 mg/L, indicated that some of them exhibited good activities toward various plant disease fungi. Compounds 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j showed excellent inhibitory activities (100%) against Sclerotinia sclerotiorum. (Compound) 5i showed excellent inhibitory activities (100%) against Botrytis cinerea, Penicillium (italicum) and S. sclerotiorum, and also showed inhibitory activities against Xanthomonas oryzae, Pseudomonas solanacearum.