Iodized salts are widely used as mediators to promote C-H functionalization.Solvents and additives have been described as significant roles in these reactions.However,the further electrochemical investigations have ra...Iodized salts are widely used as mediators to promote C-H functionalization.Solvents and additives have been described as significant roles in these reactions.However,the further electrochemical investigations have rarely been reported.Herein,a KI mediated electrochemical annulation between acetophenones and 2-amniopyridines was developed.We revealed the effect of acids and solvents by cyclic voltammetry(CV),differential pulse voltammetry(DPV),and square wave voltammetry(SWV).The oxidation of 2-aminopyridine is inhibited at the potential window with the addition of strong acids,and the lowest oxidation potential difference of KI was obtained by utilizing EtOH as solvent.The experimental studies also show that the mixture solvent of EtOH/DMSO(9/1,volume ratio)facilitates the electrochemical cyclization due to the solubility improvement of KI.CF3SO3H has been screened as the optimal acid.A range of Imidazo[1,2-a]-pyridines have been synthesized in yields of 42%to 96%.Electrochemical investigations present that the KI mediated electrochemical reaction is probably solvent-dependence.展开更多
In order to find novel herbicidal active compounds, a series of N-（2,2-dimethyl-7-alkoxy-2,3-dihydro- benzofuran-5-yl）-2-（4-arylxoyphenoxy）propionamides was designed, prepared and evaluated for their herbicidal ac...In order to find novel herbicidal active compounds, a series of N-（2,2-dimethyl-7-alkoxy-2,3-dihydro- benzofuran-5-yl）-2-（4-arylxoyphenoxy）propionamides was designed, prepared and evaluated for their herbicidal activity. Bioassay results showed that most of the title compounds had excellent and selective herbicidal activity against the monocotyledonous grasses. In particular, compounds lg and lm showed 100% inhibition against the growth of three monocotyledonous grasses under both postemergence and preemergence treatments at the dose of 2250 g/hm2 （1 hm2= 104 m2）, and could be used as lead compounds for further development of novel potential herbicidal agents.展开更多
A series of novel thiazole Schiff base derivatives containing benzo[d][1,3]dioxole moiety was designed, synthesized and screened for their fungicidal activities. The preliminary results demonstrated that compounds 6p,...A series of novel thiazole Schiff base derivatives containing benzo[d][1,3]dioxole moiety was designed, synthesized and screened for their fungicidal activities. The preliminary results demonstrated that compounds 6p, 6q and 6r possessed potent activities against Phytophthora infestans, Pyricularia oryzae and Septoria tritici in vitro. Compounds 6d and 6r exhibited remarkable activities against Botrytis cinerea（whole plant） and Phytophthora in- festans（leaf disk） respectively in vivo, which were identified as the most promising candidates for further study and could be used as possible lead compounds for developing new fungicides.展开更多
Twenty-seven novel chaicone derivatives were designed and synthesized as neuraniinidase(NA) inhibitors. A concise suitable synthetic strategy was employed in the target compounds? synthesis with relatively high yields...Twenty-seven novel chaicone derivatives were designed and synthesized as neuraniinidase(NA) inhibitors. A concise suitable synthetic strategy was employed in the target compounds? synthesis with relatively high yields. The synthesized compounds were evaluated for their inhibitory activities against the NA of influenza A virus in vitro. The results show that compound 9b possesses the most potent NA inhibitory activity. Structure-activity relationship studies indicate that the chaicone system and hydrogen bond donor substituent are significant for the NA inhibitory activity. And the chaicone derivatives containing pyran ring have better NA inhibitory activity than those without the pyran ring. In addition, molecular docking studies reveal that compounds 9b and 9u are in the good binding mode with Zanamivir binding sites. This study indicates that compound 9b could be selected as a potent compoxind for further structural optimization and development of novel NA inhibitors.展开更多
A series of novel N-allyloxy/propargyloxy aryloxyphenoxy propionamide compounds was designed and prepared. The structures of the synthesized compounds were confirmed by means of 1H NMR, 13C NMR, LC-MS, elemental analy...A series of novel N-allyloxy/propargyloxy aryloxyphenoxy propionamide compounds was designed and prepared. The structures of the synthesized compounds were confirmed by means of 1H NMR, 13C NMR, LC-MS, elemental analysis and IR. The bioassay results indicate that when against Digitaria sanguinalis and Echinochloa crus-galli, （R）-N-（propargyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy] phenoxy}propanamide（1m）（IC50=6.8 and 6.5 g/hm2, respectively） and （R）-N-（allyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy]phenoxy}propanamide（1r）（IC50=7.4 and 6.0 g/hm2, respectively） are much more effective than commercial aryloxyphenoxypropionic ester herbicide clodinafop-propargyl（IC50=46.5 and 14.6 g/hm2, respectively）. The results of crop selectivity show that compounds 1m and 1r are safe to soybean, rape and cotton and can be used as herbicides for soybean, rape and cotton crop.展开更多
文摘Iodized salts are widely used as mediators to promote C-H functionalization.Solvents and additives have been described as significant roles in these reactions.However,the further electrochemical investigations have rarely been reported.Herein,a KI mediated electrochemical annulation between acetophenones and 2-amniopyridines was developed.We revealed the effect of acids and solvents by cyclic voltammetry(CV),differential pulse voltammetry(DPV),and square wave voltammetry(SWV).The oxidation of 2-aminopyridine is inhibited at the potential window with the addition of strong acids,and the lowest oxidation potential difference of KI was obtained by utilizing EtOH as solvent.The experimental studies also show that the mixture solvent of EtOH/DMSO(9/1,volume ratio)facilitates the electrochemical cyclization due to the solubility improvement of KI.CF3SO3H has been screened as the optimal acid.A range of Imidazo[1,2-a]-pyridines have been synthesized in yields of 42%to 96%.Electrochemical investigations present that the KI mediated electrochemical reaction is probably solvent-dependence.
文摘In order to find novel herbicidal active compounds, a series of N-（2,2-dimethyl-7-alkoxy-2,3-dihydro- benzofuran-5-yl）-2-（4-arylxoyphenoxy）propionamides was designed, prepared and evaluated for their herbicidal activity. Bioassay results showed that most of the title compounds had excellent and selective herbicidal activity against the monocotyledonous grasses. In particular, compounds lg and lm showed 100% inhibition against the growth of three monocotyledonous grasses under both postemergence and preemergence treatments at the dose of 2250 g/hm2 （1 hm2= 104 m2）, and could be used as lead compounds for further development of novel potential herbicidal agents.
文摘A series of novel thiazole Schiff base derivatives containing benzo[d][1,3]dioxole moiety was designed, synthesized and screened for their fungicidal activities. The preliminary results demonstrated that compounds 6p, 6q and 6r possessed potent activities against Phytophthora infestans, Pyricularia oryzae and Septoria tritici in vitro. Compounds 6d and 6r exhibited remarkable activities against Botrytis cinerea（whole plant） and Phytophthora in- festans（leaf disk） respectively in vivo, which were identified as the most promising candidates for further study and could be used as possible lead compounds for developing new fungicides.
基金the Hunan Provincial Natural Science Foundation,China(No.2019JJ40030)the National Natural Science Foundation of China(No.81673480).
文摘Twenty-seven novel chaicone derivatives were designed and synthesized as neuraniinidase(NA) inhibitors. A concise suitable synthetic strategy was employed in the target compounds? synthesis with relatively high yields. The synthesized compounds were evaluated for their inhibitory activities against the NA of influenza A virus in vitro. The results show that compound 9b possesses the most potent NA inhibitory activity. Structure-activity relationship studies indicate that the chaicone system and hydrogen bond donor substituent are significant for the NA inhibitory activity. And the chaicone derivatives containing pyran ring have better NA inhibitory activity than those without the pyran ring. In addition, molecular docking studies reveal that compounds 9b and 9u are in the good binding mode with Zanamivir binding sites. This study indicates that compound 9b could be selected as a potent compoxind for further structural optimization and development of novel NA inhibitors.
基金Supported by the National Natural Science Foundation of China（No.21272062）, the Startup Foundation of China Three Gorges University（No.KJ2014B084） and the Open Foundation of Hubei Key Laboratory of Tumor Microenvironment and Im- munotherapy, China（No.2015KZL09）.
文摘A series of novel N-allyloxy/propargyloxy aryloxyphenoxy propionamide compounds was designed and prepared. The structures of the synthesized compounds were confirmed by means of 1H NMR, 13C NMR, LC-MS, elemental analysis and IR. The bioassay results indicate that when against Digitaria sanguinalis and Echinochloa crus-galli, （R）-N-（propargyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy] phenoxy}propanamide（1m）（IC50=6.8 and 6.5 g/hm2, respectively） and （R）-N-（allyloxy）-2-{4-[（6-chloroquinoxalin-2-yl） oxy]phenoxy}propanamide（1r）（IC50=7.4 and 6.0 g/hm2, respectively） are much more effective than commercial aryloxyphenoxypropionic ester herbicide clodinafop-propargyl（IC50=46.5 and 14.6 g/hm2, respectively）. The results of crop selectivity show that compounds 1m and 1r are safe to soybean, rape and cotton and can be used as herbicides for soybean, rape and cotton crop.
