In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and syn...In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-lH-pyr- azole-5-carboxylate 1 as starting materials. N-Methyl-3-alkyl-4-amino-lH-pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-lH-pyrazole-5-carboxyl chlorides 4a, 4b, lla, llb, llc or 12 were also obtained from 1 via several steps. Target compounds 7a-Tg were obtained after the reaction of 6 with the above 1H-pyrazole-5-carboxyl chlorides. Preliminary bioassay showed some compounds possessing good inactivation effect against TMV （tobacco mosaic virus）. Compound 7a showed higher activity superior to ningnanmycin at a concentration of 5.0 × 10^-4 g/mE and equal activity at 1.0 × 10^-4 g/mE; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10^-4 g/mE and 1.0 × 10^-4 g/mL.展开更多
In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitutio...In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitution, reduction and acylation procedures. Preliminary bioassay showed that all the target compounds processing good anti-TMV （tobacco mosaic virus） activity. Two compounds （4d and 4e） displayed higher activity superior to virazole at a concentration of 5.0 ×10^-4 g/mE.展开更多
基金the National Natural Science Fund of China(No.20902107)the Fundamental Research Fund for the Central Universities(No.2011JS033)
文摘In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-lH-pyr- azole-5-carboxylate 1 as starting materials. N-Methyl-3-alkyl-4-amino-lH-pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-lH-pyrazole-5-carboxyl chlorides 4a, 4b, lla, llb, llc or 12 were also obtained from 1 via several steps. Target compounds 7a-Tg were obtained after the reaction of 6 with the above 1H-pyrazole-5-carboxyl chlorides. Preliminary bioassay showed some compounds possessing good inactivation effect against TMV （tobacco mosaic virus）. Compound 7a showed higher activity superior to ningnanmycin at a concentration of 5.0 × 10^-4 g/mE and equal activity at 1.0 × 10^-4 g/mE; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10^-4 g/mE and 1.0 × 10^-4 g/mL.
基金the the National 11th-Five-year Science and Technology Support Project on Pesticide Innovation (No.2006BAE01A01-1104)National Natural Science Foundation of China(No.20672138+1 种基金No.20902107)the Research Innovation Foundation of China Agricultural University(No.2006009)
文摘In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitution, reduction and acylation procedures. Preliminary bioassay showed that all the target compounds processing good anti-TMV （tobacco mosaic virus） activity. Two compounds （4d and 4e） displayed higher activity superior to virazole at a concentration of 5.0 ×10^-4 g/mE.
