Synthesis And Antifungal Activity Of Novel Triazole Compounds

Due to possessing excellent biological activity, especially its high efficacy and broad spectrum of action, Triazoles pesticides has always attracted researchers’ considerable attention. On the other hand, Designing novel structure triazoles for new pesticide discovery has practical significance since the drug resistance of triazoles fungicide in recent years. Coumarin compounds with bactericidal activity, herbicidal activity and significant biological activity are also important benzoheterocyclic compounds. Our group envisages combing Coumarin with advantage of structure of triazoles heterocyclic derivatives to develope a target molecule possessing novel structure and higher activity. Hence, based on active group split and bioisosteric principle, To design synthesis A, B, C three series has novel structure of new type three azole antifungal compounds, And the synthesis of coumarin and A series of compound process optimization. and has made the antifungal activity of three kinds of compounds. This thesis is divided into the following two parts:1. a-bromoacetophenone,1,2,4-triazole and 3,4,6-substituted 7-hydroxycoumarin as starting materials, we synthesize a series of A compounds via multi-steps, and the optimization of synthetic conditions on the technology; 1-Chloropinacolone,1,2,4-triazole and 3,4,6-substituted 7-hydroxycoumarin as starting materials; we synthesize a series of A compounds via multi-steps; salicylaldehyde, ethyl acetoacetate, ethylene glycol 1,2,4-triazole and 3,4,6-substituted 7-hydroxycoumarin as starting materials, We synthesize a series of C compounds via multi-steps;All the target products were characterized via IR、1H-NMR、 13C-NMR、LC-MS methods.2. Antimicrobial activity test experiments with Fusarium graminearum Schw、Botrytis cinerea Pers.Ex Fr、Thanatephorus cucumeris (Frank) Donk as a test species and triazolone fungicide as a positive control, we test synthesized three series A, B, C triazole fungicides antimicrobial activity under 125mg/L of drug concentration, After tests found that compounds of three kinds of pathogenic bacteria have inhibition effect, part of the compound bactericidal effect is better than the positive control triadimefon, coumarin on the aromatic ring to the substituent of the compounds than has electron-withdrawing substituent of the compounds.