（S）-（＋）-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of dehydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial...（S）-（＋）-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of dehydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of （S）-（＋）-2,2-dimethylcyclopropane carbox amide in toluene, dichloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured using the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation.The calculated values were good in agreement with the experimental values.展开更多
(S)-(+)-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of de- hydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial de...(S)-(+)-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of de- hydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of (S)-(+)-2,2-dimethylcyclopropane carbox amide in toluene, di- chloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured us- ing the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation. The calculated values were good in agreement with the experimental values.展开更多
The polycondensation of the mixture of diamines 5,5-methylene bis(2-aminophenol) and 4,4-(hexafluoroisopropylidene)dianiline(molar ratio 0.8:0.2) with isophthaloyl dichloride was used to synthesize poly(amido-o-hydrox...The polycondensation of the mixture of diamines 5,5-methylene bis(2-aminophenol) and 4,4-(hexafluoroisopropylidene)dianiline(molar ratio 0.8:0.2) with isophthaloyl dichloride was used to synthesize poly(amido-o-hydroxy amide)(POA-F)-new heat resistant binder of the composites for microelectronics. The copolymer was fractionated, its hydrodynamic, optical, and conformational properties were researched, and molecular masses(ММ) of the fractions were defined. The polydispersity index was estimated. Based on experimental data, calculation of the size of a segment of Kuhn characterizing degree of an intramolecular orientation order and value of coefficients of the equation of Mark-Kuhn-Hauvink for viscometric and diffusion data were performed. It was demonstrated that introducing 20 mol % of the monomer with-CF3-groups does not lead to any changes in conformational properties of the macromolecules and does not change the degree of intramolecular orientational order(the Kuhn segment length). Optical characteristics of POA-F solutions are virtually similar to the corresponding values for POA prepared with the use of single amine-containing component-5,5-methylene bis(2-aminophenol). The received MM distribution for POA-F(prepolymer) provided the solubility of its films in alkaline solutions. The heat resistance(τ5 and τ10-temperatures corresponding to 5% and of 10% PBO-F mass loss of a polymer) of the powders and the films of PBO, PBO-F were determined. The electrophysical parameters-dielectric permittivity(ε) and dielectric loss tangent(tan δ) of the PBO-F films decreased down to 3.30 and 0.017, in comparison 3.40 and 0.025 for PBO respectively.展开更多
Lithium aluminium amide [LiAI（NHR）4] 5 obtained by treating the primary amine 4 with LiAlH4 could promote the ring opening of epoxide 2 and led to high regioselective product of racemic bis[2-（6-fluoro-2-chromanyl...Lithium aluminium amide [LiAI（NHR）4] 5 obtained by treating the primary amine 4 with LiAlH4 could promote the ring opening of epoxide 2 and led to high regioselective product of racemic bis[2-（6-fluoro-2-chromanyl）-2-hydroxyethyl]amine methanesulfonic acid salt 7.展开更多
Chiral 4-[(2-isopropyl-5-methylcyclohexyl)oxo]-4-oxobutanoic acid reacts with substituted anilines to produce amides 1-6 in high yields. Resulted amides 1-6 were investigated for their antifungal and antibacterial act...Chiral 4-[(2-isopropyl-5-methylcyclohexyl)oxo]-4-oxobutanoic acid reacts with substituted anilines to produce amides 1-6 in high yields. Resulted amides 1-6 were investigated for their antifungal and antibacterial activities. Compounds 2 (96.5%) against Aspergillus fumigatus and 6 (93.7%) against Helminthosporium sativum demonstrated excellent activities. However, compounds 3 (37.6%) against Bacillus subtilis, 4 (33.2%) against Pseudomonas aurignosa, 5 against Klebsiella pneumonia demonstrated excellent growth inhibition potential.展开更多
The esterifications of 9-（hydroxyimino）-4-methyl-8,9-dihydrofuro[2,3-h]chromen-2-one （4） with acid chlorides afforded normal oxime-esters 3a-e in 35-78% yields in presence of excessive 4-dimethylaminopyridine as t...The esterifications of 9-（hydroxyimino）-4-methyl-8,9-dihydrofuro[2,3-h]chromen-2-one （4） with acid chlorides afforded normal oxime-esters 3a-e in 35-78% yields in presence of excessive 4-dimethylaminopyridine as the acid scavenger, whereas the reactions gave unexpected 8-substituted products N-（8-chloro-4-methyl-2-oxo-2H-furo-[2,3-h]chromen-9-yl）amides （5a-c） and 4-methyl-2,9-dioxo-8,9-dihydro-2H-furo[2,3-h]chromen-8-ylcarboxyloates （6d-e） by using excessive acid chlorides. The structures of 10 new compounds were determined by 1H NMR, 13C NMR, MS and HRMS, and the possible mechanism for the formation of unexpected products 5a--c and 6d-e was also proposed.展开更多
A variety of new N-(5-(benzofuranol-7-oxymethyl)-1,3,4-thiadiazol-2-yl)amide compounds(8a-i)were synthesized through four steps from benzofuranol as raw materials.The crystal structure of compound 8a(C17H21N3O3S,Mr=34...A variety of new N-(5-(benzofuranol-7-oxymethyl)-1,3,4-thiadiazol-2-yl)amide compounds(8a-i)were synthesized through four steps from benzofuranol as raw materials.The crystal structure of compound 8a(C17H21N3O3S,Mr=347.43)was measured by X-ray diffraction,which was classified as monoclinic system,Z=4,V=1742.72(8)Å3,Dc=1.324 Mg/m3,F(000)=736,S=1.03,μ=0.21 mm-1,space group P21 with a=9.9177(3),b=8.9519(2),c=19.8679(5)Å,the final R=0.035 and wR=0.105 for 3873 observed reflections(I>2σ(I)).The X-ray structure presented N(3)-H(3)···N(2)and C(6)-H(6)···O(3)intermolecular hydrogen bonds,which acted as an important role in stabilizing the crystal structure.Additionally,preliminary biological assay on compound 8a showed good fungicidal activity in vivo,with the inhibition of 75%against Pseudoperonospora cu-bensis at 200 mg/L.展开更多
Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested an...Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested and compared. The title compounds Schiff bases, amides,imidazolo[2,1-b]-1,3,4-thiadiazoles and 7H-s-triazolo [3,4-b]-1,3,4-thiadiazines have been confirmedby elemental analyses, ~1H NMR, IR and MS spectra. All the compounds have also been screened fortheir antibacterial activities against B. subtilis, S. aureus and E. coli.展开更多
文摘（S）-（＋）-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of dehydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of （S）-（＋）-2,2-dimethylcyclopropane carbox amide in toluene, dichloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured using the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation.The calculated values were good in agreement with the experimental values.
文摘(S)-(+)-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of de- hydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of (S)-(+)-2,2-dimethylcyclopropane carbox amide in toluene, di- chloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured us- ing the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation. The calculated values were good in agreement with the experimental values.
基金Funded by the Ministry of Education and Science of the Russian Federation(No.10.7608.2017/8.9).
文摘The polycondensation of the mixture of diamines 5,5-methylene bis(2-aminophenol) and 4,4-(hexafluoroisopropylidene)dianiline(molar ratio 0.8:0.2) with isophthaloyl dichloride was used to synthesize poly(amido-o-hydroxy amide)(POA-F)-new heat resistant binder of the composites for microelectronics. The copolymer was fractionated, its hydrodynamic, optical, and conformational properties were researched, and molecular masses(ММ) of the fractions were defined. The polydispersity index was estimated. Based on experimental data, calculation of the size of a segment of Kuhn characterizing degree of an intramolecular orientation order and value of coefficients of the equation of Mark-Kuhn-Hauvink for viscometric and diffusion data were performed. It was demonstrated that introducing 20 mol % of the monomer with-CF3-groups does not lead to any changes in conformational properties of the macromolecules and does not change the degree of intramolecular orientational order(the Kuhn segment length). Optical characteristics of POA-F solutions are virtually similar to the corresponding values for POA prepared with the use of single amine-containing component-5,5-methylene bis(2-aminophenol). The received MM distribution for POA-F(prepolymer) provided the solubility of its films in alkaline solutions. The heat resistance(τ5 and τ10-temperatures corresponding to 5% and of 10% PBO-F mass loss of a polymer) of the powders and the films of PBO, PBO-F were determined. The electrophysical parameters-dielectric permittivity(ε) and dielectric loss tangent(tan δ) of the PBO-F films decreased down to 3.30 and 0.017, in comparison 3.40 and 0.025 for PBO respectively.
基金the National 863 Program(No.2003AA323030)the National Natural Science Foundation of China(No.50272069 and No.20472090)for financial support.
文摘Lithium aluminium amide [LiAI（NHR）4] 5 obtained by treating the primary amine 4 with LiAlH4 could promote the ring opening of epoxide 2 and led to high regioselective product of racemic bis[2-（6-fluoro-2-chromanyl）-2-hydroxyethyl]amine methanesulfonic acid salt 7.
文摘Chiral 4-[(2-isopropyl-5-methylcyclohexyl)oxo]-4-oxobutanoic acid reacts with substituted anilines to produce amides 1-6 in high yields. Resulted amides 1-6 were investigated for their antifungal and antibacterial activities. Compounds 2 (96.5%) against Aspergillus fumigatus and 6 (93.7%) against Helminthosporium sativum demonstrated excellent activities. However, compounds 3 (37.6%) against Bacillus subtilis, 4 (33.2%) against Pseudomonas aurignosa, 5 against Klebsiella pneumonia demonstrated excellent growth inhibition potential.
基金grants from the National Natural Science Foundation of China (No.20272010 and 20672022)
文摘The esterifications of 9-（hydroxyimino）-4-methyl-8,9-dihydrofuro[2,3-h]chromen-2-one （4） with acid chlorides afforded normal oxime-esters 3a-e in 35-78% yields in presence of excessive 4-dimethylaminopyridine as the acid scavenger, whereas the reactions gave unexpected 8-substituted products N-（8-chloro-4-methyl-2-oxo-2H-furo-[2,3-h]chromen-9-yl）amides （5a-c） and 4-methyl-2,9-dioxo-8,9-dihydro-2H-furo[2,3-h]chromen-8-ylcarboxyloates （6d-e） by using excessive acid chlorides. The structures of 10 new compounds were determined by 1H NMR, 13C NMR, MS and HRMS, and the possible mechanism for the formation of unexpected products 5a--c and 6d-e was also proposed.
基金supported by the Scientific Research Foundation of Hebei Educational Committee (No. QN2019058)Natural Science Foundation of Hebei Province of China (No. H2021201059)
文摘A variety of new N-(5-(benzofuranol-7-oxymethyl)-1,3,4-thiadiazol-2-yl)amide compounds(8a-i)were synthesized through four steps from benzofuranol as raw materials.The crystal structure of compound 8a(C17H21N3O3S,Mr=347.43)was measured by X-ray diffraction,which was classified as monoclinic system,Z=4,V=1742.72(8)Å3,Dc=1.324 Mg/m3,F(000)=736,S=1.03,μ=0.21 mm-1,space group P21 with a=9.9177(3),b=8.9519(2),c=19.8679(5)Å,the final R=0.035 and wR=0.105 for 3873 observed reflections(I>2σ(I)).The X-ray structure presented N(3)-H(3)···N(2)and C(6)-H(6)···O(3)intermolecular hydrogen bonds,which acted as an important role in stabilizing the crystal structure.Additionally,preliminary biological assay on compound 8a showed good fungicidal activity in vivo,with the inhibition of 75%against Pseudoperonospora cu-bensis at 200 mg/L.
文摘Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested and compared. The title compounds Schiff bases, amides,imidazolo[2,1-b]-1,3,4-thiadiazoles and 7H-s-triazolo [3,4-b]-1,3,4-thiadiazines have been confirmedby elemental analyses, ~1H NMR, IR and MS spectra. All the compounds have also been screened fortheir antibacterial activities against B. subtilis, S. aureus and E. coli.
