N-烃氧羰基-2-噻唑烷酮衍生物的合成及其杀菌活性

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

摘要: 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1H NMR、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Sclerotinia sclerotiorum的抑制率为100%, 5i 对番茄灰霉病菌Botrytis cinerea、柑桔青霉病菌Penicillium italicum和油菜菌核病菌的抑制率均为100%。

Abstract: 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.