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
N-Methylimidazolium perchlorate（[MIm]ClO_4） was synthesized and some of its physico-chemical properties, such as density, surface tension were investigated. A thermo gravimetric analysis（TGA） and solvent performan...N-Methylimidazolium perchlorate（[MIm]ClO_4） was synthesized and some of its physico-chemical properties, such as density, surface tension were investigated. A thermo gravimetric analysis（TGA） and solvent performance were also studied. The results show that this ionic liquid is an excellent catalyst for the synthesis of 4,4＇-（arylmethylene）bis（1H-pyrazol-5-ol） derivatives under solvent-free conditions.This method has the advantages of high yield, clean transformation, simple operation and short reaction time. The ionic liquid can be recycled without significant loss of activity.展开更多
The reactions of the mixture of 1- and 2-[2,2-bis（3,5-dimethylpyrazol-l-yl）-1-phenylethyl]-1,3-cyclopentadiene （bpzpcpH） and mixture of 1- and 2-[2,2-bis（3,5-dimethylpyrazol-l-yl）-I,l-diphenylethyl]-l,3-cyclopen...The reactions of the mixture of 1- and 2-[2,2-bis（3,5-dimethylpyrazol-l-yl）-1-phenylethyl]-1,3-cyclopentadiene （bpzpcpH） and mixture of 1- and 2-[2,2-bis（3,5-dimethylpyrazol-l-yl）-I,l-diphenylethyl]-l,3-cyclopentadiene （bpzdpcpH） with W（CO）sTHF have been carried out. The former yields complex （bpzpcpH）W（CO）4, in which the bpzpcpH acts as a k2-（N,N） bidentate ligand, and the cyclopentadiene moiety does not participate in the coordination to the tungsten atom. While the latter gives complex （bpzdpcpH）W（CO）3, in which the cyclopentadiene moiety coordinates to the tungsten atom in η2-fashion instead of general η5-coordinated mode, causing bpzdpcpH to act as a tridentate k3-（π,N,N） ligand,展开更多
The reaction of triphenylstannyl-bis(3,5-dimethyl-4-ethylpyrazol-1-yl)methane with W(CO)5THF yields the title compound (C37.5H39.5N4O3SnW, Mr = 896.79) which is of triclinic, space group P with a = 9.755(3), b = 13.69...The reaction of triphenylstannyl-bis(3,5-dimethyl-4-ethylpyrazol-1-yl)methane with W(CO)5THF yields the title compound (C37.5H39.5N4O3SnW, Mr = 896.79) which is of triclinic, space group P with a = 9.755(3), b = 13.696(4), c = 14.359(5) , a = 96.202(7), b = 93.313(6), g = 94.845(6)o, V = 1896(1) 3, Z = 2, Dc = 1.571 g/cm3, l(MoKa) = 0.71073 , m = 3.728 mm-1, F(000) = 881, R = 0.0491 and wR = 0.0856 for 4242 observed reflections (I≥2s(I)). The crystal structural analysis indicates that bis(3,5-dimethyl-4-ethylpyrazol-1-yl)methide acts as a tridentate monoanionic k3-[N,C,N] chelating ligand, and four-membered metallacycles are found in this heterodinuclear complex.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 partial support from University Malaya to Project GC 001A-14-AET
文摘N-Methylimidazolium perchlorate（[MIm]ClO_4） was synthesized and some of its physico-chemical properties, such as density, surface tension were investigated. A thermo gravimetric analysis（TGA） and solvent performance were also studied. The results show that this ionic liquid is an excellent catalyst for the synthesis of 4,4＇-（arylmethylene）bis（1H-pyrazol-5-ol） derivatives under solvent-free conditions.This method has the advantages of high yield, clean transformation, simple operation and short reaction time. The ionic liquid can be recycled without significant loss of activity.
基金Project supported by the National Natural Science Foundation of China （No. 20672059）.
文摘The reactions of the mixture of 1- and 2-[2,2-bis（3,5-dimethylpyrazol-l-yl）-1-phenylethyl]-1,3-cyclopentadiene （bpzpcpH） and mixture of 1- and 2-[2,2-bis（3,5-dimethylpyrazol-l-yl）-I,l-diphenylethyl]-l,3-cyclopentadiene （bpzdpcpH） with W（CO）sTHF have been carried out. The former yields complex （bpzpcpH）W（CO）4, in which the bpzpcpH acts as a k2-（N,N） bidentate ligand, and the cyclopentadiene moiety does not participate in the coordination to the tungsten atom. While the latter gives complex （bpzdpcpH）W（CO）3, in which the cyclopentadiene moiety coordinates to the tungsten atom in η2-fashion instead of general η5-coordinated mode, causing bpzdpcpH to act as a tridentate k3-（π,N,N） ligand,
基金the National Natural Science Foundation of China (No. 20172029)
文摘The reaction of triphenylstannyl-bis(3,5-dimethyl-4-ethylpyrazol-1-yl)methane with W(CO)5THF yields the title compound (C37.5H39.5N4O3SnW, Mr = 896.79) which is of triclinic, space group P with a = 9.755(3), b = 13.696(4), c = 14.359(5) , a = 96.202(7), b = 93.313(6), g = 94.845(6)o, V = 1896(1) 3, Z = 2, Dc = 1.571 g/cm3, l(MoKa) = 0.71073 , m = 3.728 mm-1, F(000) = 881, R = 0.0491 and wR = 0.0856 for 4242 observed reflections (I≥2s(I)). The crystal structural analysis indicates that bis(3,5-dimethyl-4-ethylpyrazol-1-yl)methide acts as a tridentate monoanionic k3-[N,C,N] chelating ligand, and four-membered metallacycles are found in this heterodinuclear complex.
