New compounds were synthesized,which belong to 3 types of pyrimidinyl(triazinyl)oxy substituted carboxylic derivatives respectively.In bioassay,the effects of the structural factors on the herbicidal activity were inv...New compounds were synthesized,which belong to 3 types of pyrimidinyl(triazinyl)oxy substituted carboxylic derivatives respectively.In bioassay,the effects of the structural factors on the herbicidal activity were investigated,in which the stereochemistry has a strong influence on the activity.展开更多
Thirteen novel phenyl substituted isoxazolecarboxamides were synthesized, and their structures were characterized by IH NMR, elementary analysis and high-resolution mass spectrometry（HRMS） techniques. Their evaluate...Thirteen novel phenyl substituted isoxazolecarboxamides were synthesized, and their structures were characterized by IH NMR, elementary analysis and high-resolution mass spectrometry（HRMS） techniques. Their evaluated insecticidal activities against oriental armyworm（Mythimna separata） indicate that the phenyl substituted isoxazolecarboxamides exhibited moderate insecticidal activities, among which compounds 9c and 9k showed com- paratively higher activities.展开更多
Sulfonylurea herbicides have been applied worldwide in agriculture. Some sulfonylurea residues might exist in soil longer than that people expected. However, flupyrsulfuron-methyl-sodium which was firstly reported as ...Sulfonylurea herbicides have been applied worldwide in agriculture. Some sulfonylurea residues might exist in soil longer than that people expected. However, flupyrsulfuron-methyl-sodium which was firstly reported as a new 5-substituted sulfonylurea herbicide has less than one month residual life. Therefore, 5-substituted benzenesulfonylureas are potential molecules to regulate its residual situation. In order to develop new sulfonylurea derivatives, the substituent on the critical 5-posotion of the benzene ring was optimized. On the basis of our former work on sulfonylureas which contains a characteristic mono-substituted pyrimidine moiety, twenty-six new sulfonylurea deriva- tives were synthesized and their structures were confirmed by 1H NMR, 31p NMR and elemental analysis. The greenhouse bioassay tests show that some title compounds exhibit potent herbicidal activity.展开更多
Nine new a-aminophosphonate derivatives containing cyclopropane moiety have been synthesized via conventional and microwave irradiation methods under solvent- and catalyst-free condition. The structures of the title c...Nine new a-aminophosphonate derivatives containing cyclopropane moiety have been synthesized via conventional and microwave irradiation methods under solvent- and catalyst-free condition. The structures of the title compounds have been confirmed by ^1H NMR, ^31p NMR FTIR, EI-MS and FTICR-MS. Their antifungal activities were evaluated in vivo and some of the compounds were found to exhibit excellent antifungal activities against Corynespora cassiicola, Pseudomonas syringae pv. Lachrymans, Pseudoperonospora cubensis and Sclerotinia sclerotiorum.展开更多
wenty-eight new N-2-thiazolyl and thiazolinyl-N'-substituted phenylureaswere synthesized by the reaction of the heterocycles and substituted phenyl iso-cyanates. Their cytokinin activity was examined by cucumber c...wenty-eight new N-2-thiazolyl and thiazolinyl-N'-substituted phenylureaswere synthesized by the reaction of the heterocycles and substituted phenyl iso-cyanates. Their cytokinin activity was examined by cucumber cotyledon expansionbioassay. N-thiazolyl and N-thiazolinyl-N'-(m-chlorophenyl )-ureas showed a goodPGR activity in comparison to Kinetin. The structure/activity relationship was dis-cussed.展开更多
he quantitative studies on structure and cytokinin activity of the cucumber cotyledon expansion reiationshps of 35 urea compounds were conducted using pl1ysico-chemical parameters of the substituents and regression an...he quantitative studies on structure and cytokinin activity of the cucumber cotyledon expansion reiationshps of 35 urea compounds were conducted using pl1ysico-chemical parameters of the substituents and regression analysis,The position-specific hydrophobic,steric and electronic effects of substituents are important to the activity.A certain overlap of the optimum conformation of the ureido structure over Kinetin was observed.The coplanarity is discussed.展开更多
A series of novel anthranilic diamides containing N-substituted arylmethyl moieties was designed and synthesized, in which the bond distance and conjugation pattern between pyrazole and pyridine rings contained in Chl...A series of novel anthranilic diamides containing N-substituted arylmethyl moieties was designed and synthesized, in which the bond distance and conjugation pattern between pyrazole and pyridine rings contained in Chlorantraniliprole were changed. Their structures were confirmed by JH NMR, IR, elemental analysis or high resolution mass spectromentry{HRMS）, and the conformation of compound 4d was confirmed by X-ray diffraction. The preliminary bioassay results indicate that all the target compounds exhibited moderate insecticidal activity against oriental armyworm at 200 mg/L and some of them presented favorable antitumor activities against human lung cancer cells（A549）, liver cancer cells（BelT402） and colon cancer celIs（HCT-8） in vitro by microculture tetrazolium（MTT） method, among which compound 6j afforded the best anti-proliferative activity at 5μg/mL.展开更多
文摘New compounds were synthesized,which belong to 3 types of pyrimidinyl(triazinyl)oxy substituted carboxylic derivatives respectively.In bioassay,the effects of the structural factors on the herbicidal activity were investigated,in which the stereochemistry has a strong influence on the activity.
基金Supported by the National Natural Science Foundation of China(No. 20872069)the National Basic Research Program of China(No.2010CB126106)the Fund of State Key Laboratory of Elemento-Organic Chemistry,China
文摘Thirteen novel phenyl substituted isoxazolecarboxamides were synthesized, and their structures were characterized by IH NMR, elementary analysis and high-resolution mass spectrometry（HRMS） techniques. Their evaluated insecticidal activities against oriental armyworm（Mythimna separata） indicate that the phenyl substituted isoxazolecarboxamides exhibited moderate insecticidal activities, among which compounds 9c and 9k showed com- paratively higher activities.
基金Supported by the National Basic Research Program of China(No2010CB126106)
文摘Sulfonylurea herbicides have been applied worldwide in agriculture. Some sulfonylurea residues might exist in soil longer than that people expected. However, flupyrsulfuron-methyl-sodium which was firstly reported as a new 5-substituted sulfonylurea herbicide has less than one month residual life. Therefore, 5-substituted benzenesulfonylureas are potential molecules to regulate its residual situation. In order to develop new sulfonylurea derivatives, the substituent on the critical 5-posotion of the benzene ring was optimized. On the basis of our former work on sulfonylureas which contains a characteristic mono-substituted pyrimidine moiety, twenty-six new sulfonylurea deriva- tives were synthesized and their structures were confirmed by 1H NMR, 31p NMR and elemental analysis. The greenhouse bioassay tests show that some title compounds exhibit potent herbicidal activity.
基金Supported by the National Basic Research Program of China(No.2010B12606)
文摘Nine new a-aminophosphonate derivatives containing cyclopropane moiety have been synthesized via conventional and microwave irradiation methods under solvent- and catalyst-free condition. The structures of the title compounds have been confirmed by ^1H NMR, ^31p NMR FTIR, EI-MS and FTICR-MS. Their antifungal activities were evaluated in vivo and some of the compounds were found to exhibit excellent antifungal activities against Corynespora cassiicola, Pseudomonas syringae pv. Lachrymans, Pseudoperonospora cubensis and Sclerotinia sclerotiorum.
文摘wenty-eight new N-2-thiazolyl and thiazolinyl-N'-substituted phenylureaswere synthesized by the reaction of the heterocycles and substituted phenyl iso-cyanates. Their cytokinin activity was examined by cucumber cotyledon expansionbioassay. N-thiazolyl and N-thiazolinyl-N'-(m-chlorophenyl )-ureas showed a goodPGR activity in comparison to Kinetin. The structure/activity relationship was dis-cussed.
文摘he quantitative studies on structure and cytokinin activity of the cucumber cotyledon expansion reiationshps of 35 urea compounds were conducted using pl1ysico-chemical parameters of the substituents and regression analysis,The position-specific hydrophobic,steric and electronic effects of substituents are important to the activity.A certain overlap of the optimum conformation of the ureido structure over Kinetin was observed.The coplanarity is discussed.
文摘A series of novel anthranilic diamides containing N-substituted arylmethyl moieties was designed and synthesized, in which the bond distance and conjugation pattern between pyrazole and pyridine rings contained in Chlorantraniliprole were changed. Their structures were confirmed by JH NMR, IR, elemental analysis or high resolution mass spectromentry{HRMS）, and the conformation of compound 4d was confirmed by X-ray diffraction. The preliminary bioassay results indicate that all the target compounds exhibited moderate insecticidal activity against oriental armyworm at 200 mg/L and some of them presented favorable antitumor activities against human lung cancer cells（A549）, liver cancer cells（BelT402） and colon cancer celIs（HCT-8） in vitro by microculture tetrazolium（MTT） method, among which compound 6j afforded the best anti-proliferative activity at 5μg/mL.
