Lewis acid La(OTf) 3 -catalyzed chemoselective cyclization of hydroxyl substituted ethylenediamine derivatives with aldehydes has been described for the first time, which provides efficient access to diversely functionalized 1,3-imidazoli-dines and 3,1-benzoxazines in generally good yields only by adjusting the position of the methylene group within hydroxyl substituted ethylenediamines. The reaction is suitable to aromatic aldehydes and aliphatic ones. Plausible mechanisms are also proposed to explain the observed reaction modes, wherein the nucleophilicity of nitrogen and oxygen atoms plays an important role in controlling the chemoselectivity.

A series of novel 2-hydroxyphenyl substituted aminoacetamides was designed by molecular hybridization of the aminoacetamide scaffold and 2-hydroxyphenyl motif. The target compounds were synthesized and their fungicidal activities were evaluated. Some of the target compounds showed excellent antifungal activities against S. sclerotiorum and P. capsici. Significantly, compounds 5e displayed the most potent activity against S. sclerotiorum with EC50 = 2.89 µg/mL, which was lower than that of commercial chlorothalonil. The systematic studies provided strong confidence that the hydroxyl group and the carbonyl group are crucial for the fungicidal activity. Molecular docking studies suggest that SDH enzyme could be one of the potential action targets of our compounds.

2-Aminobenzyl alcohol and its derivatives are a kind of important bifunctional compounds,and has found wide application in organic chemistry and drug synthesis.An efficient and simple method for synthesis of 2-(arylaminoethylamino) benzyl alcohols was described and the fungicidal activities of the target compounds were evaluated in this paper.N-alkylation of 2-aminobenzyl alcohol with bromoacetyl aryl amines produced 2-[(2-hydroxymethylphenyl)amino] acetyl aryl amines 3a ～3i,which were reduced by LiAlH4 giving a series of novel 2-(arylaminoethylamino) benzyl alcohols 5a ～ 5i in 76％ ～ 95％ yields.All the structures of the target compounds were characterized by the infrared spectroscopy (IR),proton nuclear magnetic resonance spectroscopy (1H NMR),13C NMR and elemental analysis.Most of compounds show moderate to good fungicidal activities under the testing concentration.Compound 5e shows 73％ activity of against Phytophythora capsici.

首次对2-(2-硝基苯基)-3-(4甲基苯基)-1,3-苯并噁嗪(1)与利什曼原虫CYP51的相互作用进行了初步研究,发现化合物1对利什曼原虫CYP51表现出较强的抑制活性,且作用方式类似于底物与利什曼原虫CYP51的Ⅰ型结合方式.该研究不仅发现了一种新型非唑类针对利什曼原虫CYP51的抑制剂:1,3-苯并噁嗪,而且也为创制新型作用方式的CYP51抑制剂研究提供了依据.

A series of novel trans-2,3,6(8)-trisubstituted-1,3-benzoxazines were prepared in yields of 38%similar to 80% by reactions of 2-arylaminomethyl phenols with various substituted benzaldehydes in the presence of TMSCl. The reaction showed high trans selectivity. The structures of all the target products were characterized by H-1 NMR, C-13 NMR, IR and elemental analysis. The fungicidal activities of the prepared compounds were investigated, most of which showed moderate to good activity, compounds 5d and 5f showed growth inhibition of 78.6% against M oryzae at 50 mu g/mL.