Four 1, 2,3,4-tetrahydro - β - c arboline amino acid esters with a heterocycle at the C- 1position were used as chiral ligands in the enantioselective addition reactions. The differentpositions of the heteroatoms gav...Four 1, 2,3,4-tetrahydro - β - c arboline amino acid esters with a heterocycle at the C- 1position were used as chiral ligands in the enantioselective addition reactions. The differentpositions of the heteroatoms gave different effects, and medium but opposite enantioselectivitywas recorded.展开更多
A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized fr...A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry(MS) and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.展开更多
3,5,6,8-Tetrahydro-4H-thiopyrano[4',3':4,5]thieno[2,3-d]pyrimidin-4-ones(7) were synthesized via the base catalytic reactions of amines or phenols with carbodiimides(5), which were obtained from the aza-Wittig ...3,5,6,8-Tetrahydro-4H-thiopyrano[4',3':4,5]thieno[2,3-d]pyrimidin-4-ones(7) were synthesized via the base catalytic reactions of amines or phenols with carbodiimides(5), which were obtained from the aza-Wittig reac tions of iminophosphoranes(4) with aromatic isocyanates.展开更多
1 Introduction In the last decades,the furazan fused ring compounds have been paid much more attention owing to their characteristics,such as high density,high specific volume and high nitrogen content.A novel energet...1 Introduction In the last decades,the furazan fused ring compounds have been paid much more attention owing to their characteristics,such as high density,high specific volume and high nitrogen content.A novel energetic compound based on furazan fused ring,6-nitroimino-4,8-dinitro-5,6,7,8-tetrahydro-4H-imidazo furazano pyrazine(NIFDNP),was firstly designed and its properties of physico-chemical and detonation were calculated by Gaussian 09 program[4] and VLW method[5].Using glyoxal展开更多
A new benzylisoquinoline alkaloid, 1, 2, 3, 4-tetrahydro-5-hydroxyl-8-methoxyl-2- methyl-4'-methoxyl-benzylisoquinoline, was isolated from the arial parts of Sabia parviflora. Its structure was established on the...A new benzylisoquinoline alkaloid, 1, 2, 3, 4-tetrahydro-5-hydroxyl-8-methoxyl-2- methyl-4'-methoxyl-benzylisoquinoline, was isolated from the arial parts of Sabia parviflora. Its structure was established on the basis of spectral analysis.展开更多
2a,4-Disubstituted 2,2a,3,4-tetrahydro-2-phenyl-1H-azeto[2,1-d][1,5]benzothiazepin-1-ones, as well as 2-substi- tuted 2,3-dihydro-3-phenylacetyl-2-styryl-benzothiazoles and 4a,6-disubstituted 3-benzyl-4a,5-dihydro-2-p...2a,4-Disubstituted 2,2a,3,4-tetrahydro-2-phenyl-1H-azeto[2,1-d][1,5]benzothiazepin-1-ones, as well as 2-substi- tuted 2,3-dihydro-3-phenylacetyl-2-styryl-benzothiazoles and 4a,6-disubstituted 3-benzyl-4a,5-dihydro-2-phenyl- 1H,6H-[1,3]oxazino[2,3-d][1,5]benzothiazepin-1-ones, were obtained from the reaction of 2,4-disubstituted 2,3-dihydro-1,5-benzothiazepines with phenylacetyl chloride in the presence of triethylamine. The mechanism for the formation of 4a,5-dihydro-1H,6H-[1,3]oxazino[2,3-d][1,5]benzothiazepin-1-ones, 2,3-dihydro-1,3-oxazin-4-one derivatives, was suggested.展开更多
文摘Four 1, 2,3,4-tetrahydro - β - c arboline amino acid esters with a heterocycle at the C- 1position were used as chiral ligands in the enantioselective addition reactions. The differentpositions of the heteroatoms gave different effects, and medium but opposite enantioselectivitywas recorded.
基金Supported by the National Science and Technology Major Projects of China(No.2009ZX09301-012)
文摘A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry(MS) and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.
基金Supported by the National Natural Science Foundation of China(No.20772041)the Key Project of Chinese Ministry of Education(No.107082)
文摘3,5,6,8-Tetrahydro-4H-thiopyrano[4',3':4,5]thieno[2,3-d]pyrimidin-4-ones(7) were synthesized via the base catalytic reactions of amines or phenols with carbodiimides(5), which were obtained from the aza-Wittig reac tions of iminophosphoranes(4) with aromatic isocyanates.
基金Foundation Research Project of National defence(B0920110051)
文摘1 Introduction In the last decades,the furazan fused ring compounds have been paid much more attention owing to their characteristics,such as high density,high specific volume and high nitrogen content.A novel energetic compound based on furazan fused ring,6-nitroimino-4,8-dinitro-5,6,7,8-tetrahydro-4H-imidazo furazano pyrazine(NIFDNP),was firstly designed and its properties of physico-chemical and detonation were calculated by Gaussian 09 program[4] and VLW method[5].Using glyoxal
基金We are greatly indebted to Professor X. H. Hu for his help in identification of the plant material and to Professors B. R. Bai and P. Su for measuring NMR spectra.
文摘A new benzylisoquinoline alkaloid, 1, 2, 3, 4-tetrahydro-5-hydroxyl-8-methoxyl-2- methyl-4'-methoxyl-benzylisoquinoline, was isolated from the arial parts of Sabia parviflora. Its structure was established on the basis of spectral analysis.
基金Project supported partly by the National Natural Science Foundation of China (No. 20272002), the Excellent Young Teachers Program and the Sci-entific Research Foundation for the Returned Oversea Chinese Scholars of Ministry of Education of China, and
文摘2a,4-Disubstituted 2,2a,3,4-tetrahydro-2-phenyl-1H-azeto[2,1-d][1,5]benzothiazepin-1-ones, as well as 2-substi- tuted 2,3-dihydro-3-phenylacetyl-2-styryl-benzothiazoles and 4a,6-disubstituted 3-benzyl-4a,5-dihydro-2-phenyl- 1H,6H-[1,3]oxazino[2,3-d][1,5]benzothiazepin-1-ones, were obtained from the reaction of 2,4-disubstituted 2,3-dihydro-1,5-benzothiazepines with phenylacetyl chloride in the presence of triethylamine. The mechanism for the formation of 4a,5-dihydro-1H,6H-[1,3]oxazino[2,3-d][1,5]benzothiazepin-1-ones, 2,3-dihydro-1,3-oxazin-4-one derivatives, was suggested.