Asymmetric alkenylation reaction of benzoxazinones with diarylethylenes catalyzed by B(C_(6)F_(5))_(3)/chiral phosphoric acid

Catalytic enantioselective alkenylation is an efficient method to construct chiral alkene molecules,but the asymmetric alkenylation of simple alkenes catalyzed by metal-free catalysts remains an elusive challenge.Herein,we reported an asymmetric alkenylation of benzoxazinones with diarylethylenes by utilizing a B(C_(6)F_(5))_(3)/chiral phosphoric acid catalyst.A broad of benzoxazinones and diarylethylenes with electron-withdrawing and electron-donating groups were tolerated(up to 95%yield and 97.5:2.5 e.r.)in the methodology under mild reaction conditions.Moreover,the synthetic utility was confirmed by the scaled-up reaction and transformations of the products.The mechanism was preliminarily explored by control reactions,nonlinear effect experiment and DFT calculations.

Research on the allelopathic potential of wheat

Objective: This paper mainly discusses the Allelopathic potential of Wheat. Methods: This paper is prepared by reviewing the latest academic literatures. Result: The green revolution in the 1960s caused an increase in the demand for food. The agricultural sector and farmers tended to spend more time on the agricultural work but the crop yield was suppressed by the weeds. Hence, the usage of herbicide insecticides, fungicides and others chemicals had been increased. Although herbicides are efficient for weed controls, the continuous uses had gradually stimulated the weeds developing an effecttive resistance to the chemicals. Wheat (Triticum aestivum L.) is known as allelopathic against crops and weeds. Allelopathy of wheat (Triticum aestivum L.) has been extensively examined for its potentials in weeds management. The allelopathic activity of wheat has been attributed to hydroxamic acids, the related compounds and phenolic acids. Therefore, it could effectively reduce herbicide uses in order to maintain an eco-friendly environment and a cost-effective weed control.

Synthesis and evaluation of some novel additives as antioxidants and corrosion inhibitors for petroleum fractions

Benzoxazinone 2 was prepared and reacted with formamide,acetamide,some primary aromatic amines and heterocyclic amines giving the corresponding quinazolone derivatives 3-15 respectively.The reaction of benzoxazinone 2 with hydrazine hydrate and phenyl hydrazine was also studied.Representative compounds of the synthesized products were evaluated as antioxidants and corrosion inhibitors for gasoline engine lubricating oil.The highest antioxidant activities were obtained with compounds 10-15.The optimum concentration recommended for these new additives was found to be 0.lg for 1L ofoil for compounds 13-15.In addition,some of the highly effective antioxidant additives,namely 10-15,were thermally analyzed by using thermogravimetric analysis （TGA） and differential thermal gravimetric analysis （DTGA） techniques and the results indicated that compounds are thermally stable and could be used under thermal conditions.Moreover,a comparison of the oxidation stability between the tested oil containing the prepared products and lubricating oil containing commercial additives was also studied.

Quantitative Structure Activity Relationship Studies of Benzoxazinone Derivative Antithrombotic Drug Using New Three-dimensional Structure Descriptors

A novel three-dimensional holographic vector of atomic interaction field（3D-HoVAIF） was used to describe the chemical structures of 23 benzoxazinone derivatives as antithrombotic drugs.Here a quantitative structure activity relationship（QSAR） model was built by partial least-squares（PLS） regression.The estimation stability and prediction ability of the model were strictly analyzed by both internal and external validations.The correlation coefficients of established PLS model,leave-one-out（LOO） cross-validation,and predicted values versus experimental ones of external samples were R2=0.899,RCV2=0.854 and Qext2=0.868,respectively.These values indicated that the built PLS model had both favorable estimation stability and good prediction capabilities.Furthermore,the satisfactory results showed that 3D-HoVAIF could preferably express the information related to the biological activity of benzoxazinone derivatives.

Chemoselective synthesis and cytotoxic activity of a series of novel benzo[1,4]oxazin-3-one derivatives

That tetraacetonitrile copper perchlorate catalyzes intramolecular amidation of arenes was found to be a new strategy for construction of nitrogen-containing heterocycles and resulted in the formation of a series of novel benzo[1,4]oxazin-3-one derivatives from N-（1,3-diphenyl-1H-1,2,4-triazol-5-yl）-2-phenoxyacetamides.This approach of heterocyclic construction proceeds in a chemoselective manner in which only benzo[1,4]oxazin-3-one derivatives were obtained by C—N bonds formation with cheap and simple copper salt catalyst under mild conditions in moderate to good yields.The biological assay of some of benzo[1,4]oxazin-3-one derivatives showed that they had moderate antiproliferative activity toward MDA-MB231 and HeLa cancer cell lines.