Aziridine derivatives of N^5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 a...Aziridine derivatives of N^5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 and 6 exhibited superior inhibitory activities（IC50：5.05 and 4.15 μmol/L, respectively） compared to the corresponding chain analogue 4（IC55=24.42 μmol/L）. The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase.展开更多
One phosphorus heterocycle compound 1, C13H13N2OPS, was synthesized by the reaction of Lawesson＇s reagent （LR） with o-phenylene diamine. The crystal belongs to the orthorhombic system, space group P212121 with a = ...One phosphorus heterocycle compound 1, C13H13N2OPS, was synthesized by the reaction of Lawesson＇s reagent （LR） with o-phenylene diamine. The crystal belongs to the orthorhombic system, space group P212121 with a = 5.5274（11）, b = 8.1603（16）, c = 28.830（6） A, V = 1300.4（4） A^3, Z = 4, Mr= 276.28, Dc = 1.411 g/cm^3, F（000） = 576,μ = 0.360 mm^-1, R = 0.0259 and wR = 0.0652 for 1414 observed reflections with I 〉 2σ（I）. While compound 2, C14H17N2O2PS, was obtained as a ring-cleavage product of compound 1. This crystal is of monoclinic system, space group P21/c with a = 9.5619（19）, b = 21.879（4）, c = 7.3618（15） A, β= 103.03（3）°, V=1500.4（5） A^3, Z = 4, Mr= 308.33, Dc = 1.365 g/cm^3, F（000） = 648,μ = 0.325 mm^-1, R = 0.0383 and wR =0.0742 for 2283 observed reflections with I 〉 2σ（I）. Phosphorus atom in each compound bonds with sulfur and carbon atoms using sp^3 hybrid orbitals, and crystals of these two compounds are formed and stabilized by intermolecular hydrogen bonds and Van der Waals＇ forces. The special structure of compound 1 leads to its good antimicrobial activity against staphylococcus aureus.展开更多
A rapid and efficient synthesis of novel dendrimer homotriptycenes is presented. The dendronized 9,10-dihydroanthracen-9-ols 4, having high electron densities in the benzene rings of the Fréchet-type dendrons, ex...A rapid and efficient synthesis of novel dendrimer homotriptycenes is presented. The dendronized 9,10-dihydroanthracen-9-ols 4, having high electron densities in the benzene rings of the Fréchet-type dendrons, exhibited in the presence of acid a quantitative transannular ring closure to the corresponding dendritic homotriptycenes. The electron-donating Fréchet-type dendrons enabled the intramolecular FC alkylation by a regioselective 1,7-elimination of H2O.展开更多
A synthesis of (2R,3aR,8aR)-6-chloro-3a-hydroxy-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indole-2-carboxylic acid methyl ester (1) was achieved. An aldol reaction with Garner aldehyde, a hydroxyl introduction by Davis re-...A synthesis of (2R,3aR,8aR)-6-chloro-3a-hydroxy-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indole-2-carboxylic acid methyl ester (1) was achieved. An aldol reaction with Garner aldehyde, a hydroxyl introduction by Davis re-agent, and a reductive intramolecular ring-closure reaction were served as the key steps. This piece of work pro-vides a new way to synthesize the analogues of hexahydropyrrolo[2,3-b]indole, starting from readily available chemical substrates and inexpensive reagents.展开更多
基金Supported by the National Natural Science Foundation of China（No.21172014）.
文摘Aziridine derivatives of N^5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 and 6 exhibited superior inhibitory activities（IC50：5.05 and 4.15 μmol/L, respectively） compared to the corresponding chain analogue 4（IC55=24.42 μmol/L）. The results suggest that the aziridine derivatives can get potential activities against nucleophilic methionine synthase.
基金This work was supported by the National Natural Science Foundation of China (20271046), Natural Science Foundation of Henan Education Department (2004150004) and Natural Foundation of Henan Province (200011500027)
文摘One phosphorus heterocycle compound 1, C13H13N2OPS, was synthesized by the reaction of Lawesson＇s reagent （LR） with o-phenylene diamine. The crystal belongs to the orthorhombic system, space group P212121 with a = 5.5274（11）, b = 8.1603（16）, c = 28.830（6） A, V = 1300.4（4） A^3, Z = 4, Mr= 276.28, Dc = 1.411 g/cm^3, F（000） = 576,μ = 0.360 mm^-1, R = 0.0259 and wR = 0.0652 for 1414 observed reflections with I 〉 2σ（I）. While compound 2, C14H17N2O2PS, was obtained as a ring-cleavage product of compound 1. This crystal is of monoclinic system, space group P21/c with a = 9.5619（19）, b = 21.879（4）, c = 7.3618（15） A, β= 103.03（3）°, V=1500.4（5） A^3, Z = 4, Mr= 308.33, Dc = 1.365 g/cm^3, F（000） = 648,μ = 0.325 mm^-1, R = 0.0383 and wR =0.0742 for 2283 observed reflections with I 〉 2σ（I）. Phosphorus atom in each compound bonds with sulfur and carbon atoms using sp^3 hybrid orbitals, and crystals of these two compounds are formed and stabilized by intermolecular hydrogen bonds and Van der Waals＇ forces. The special structure of compound 1 leads to its good antimicrobial activity against staphylococcus aureus.
基金Supported by the National Natural Science Foundation of China (Grant Nos.20572111 & 20872038)the Science and Technology Planning Project of Guang-dong Province, China (Grant No.2007A010500011)the Research Fund for the Doctoral Program of Higher Education of China (Grant No. 20060561024)
文摘A rapid and efficient synthesis of novel dendrimer homotriptycenes is presented. The dendronized 9,10-dihydroanthracen-9-ols 4, having high electron densities in the benzene rings of the Fréchet-type dendrons, exhibited in the presence of acid a quantitative transannular ring closure to the corresponding dendritic homotriptycenes. The electron-donating Fréchet-type dendrons enabled the intramolecular FC alkylation by a regioselective 1,7-elimination of H2O.
文摘A synthesis of (2R,3aR,8aR)-6-chloro-3a-hydroxy-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indole-2-carboxylic acid methyl ester (1) was achieved. An aldol reaction with Garner aldehyde, a hydroxyl introduction by Davis re-agent, and a reductive intramolecular ring-closure reaction were served as the key steps. This piece of work pro-vides a new way to synthesize the analogues of hexahydropyrrolo[2,3-b]indole, starting from readily available chemical substrates and inexpensive reagents.
