Using N-bromosuccinimide and pyridine as the oxidation system to dehydrogenate aryl substituted semicarbazide to form azo compounds is described for the first time in this paper. Nine azo compounds have been prepared ...Using N-bromosuccinimide and pyridine as the oxidation system to dehydrogenate aryl substituted semicarbazide to form azo compounds is described for the first time in this paper. Nine azo compounds have been prepared in excellent yield under mild condition. This method only. needs simple instrument and short reaction time.展开更多
A new method to tetrahydro-β-carbolines(βCs) from tryptamine is described and the aromatization of THβCs to βCs by manganese dioxide is reported for the first time in this type of compounds.
Nor-ketoagarofuran (1), one of the furanoids isolated from grnd Oil, has been Synthesed in a preprative scale in high yield from olefin 3 in 3 steps. Reaction of norketoagarofuran (1) with CH3MgI afforded 4 (2), an an...Nor-ketoagarofuran (1), one of the furanoids isolated from grnd Oil, has been Synthesed in a preprative scale in high yield from olefin 3 in 3 steps. Reaction of norketoagarofuran (1) with CH3MgI afforded 4 (2), an another naturallyoccurring tetrahydrofuran derivative.展开更多
Arenesulfonyl chloride undergoes a facile one-pot coupling reaction with active halides assisted by zinc to give the corresponding sulfones in acceptable yields.
This paper describes the direct oxidation of pyridines to pyridine-N-oxides by means of 30% H2O2 in aq media in the presence of Na2WO4.2H(2)O as catalyst instead of with per-acids or 30% H2O2 in acetic acid. Good yiel...This paper describes the direct oxidation of pyridines to pyridine-N-oxides by means of 30% H2O2 in aq media in the presence of Na2WO4.2H(2)O as catalyst instead of with per-acids or 30% H2O2 in acetic acid. Good yields were obtained.展开更多
The reaction of two series of 2,3-dihydro-1,5-henzothiazepines Ⅰ with dichloro- carbene,gave azirino[2,1-d][1,5]benzothiazepines Ⅷ,azirino[2,1-e][1,6]benzothiazocines Ⅸ, pyrrolo[2,1-b][1,3]benzothiazoles Ⅹ,substit...The reaction of two series of 2,3-dihydro-1,5-henzothiazepines Ⅰ with dichloro- carbene,gave azirino[2,1-d][1,5]benzothiazepines Ⅷ,azirino[2,1-e][1,6]benzothiazocines Ⅸ, pyrrolo[2,1-b][1,3]benzothiazoles Ⅹ,substituted-cyclopropanes Ⅺ and 2H-1,4-benzothiazin-2-ones Ⅻ.The structures of these products were confirmed by the analytical and spectral data.Compound Ⅷ and Ⅸ are two new ring systems.展开更多
A new prenylated flavonol, maackiaflavonol, was isolated from the ethanol extract of the roots of Maackia tenuifolia. Its structure was elucidated as 7-hydrox-8-prenylflavonol by means of spectroscopic analysis (UV, I...A new prenylated flavonol, maackiaflavonol, was isolated from the ethanol extract of the roots of Maackia tenuifolia. Its structure was elucidated as 7-hydrox-8-prenylflavonol by means of spectroscopic analysis (UV, IR, MS, NMR and 1H-1H COSY) and confirmed by total synthesis.展开更多
1-substituted-5-benzoylamino-4-pyrazolecarboxamides(2)were prepared by the reaction of 1-substituted pyrazolo[3,4-d]-oxazinone(1) with amines in benzene.The compound 2 was refluxed with excess LiAlH_4 in a mixture of ...1-substituted-5-benzoylamino-4-pyrazolecarboxamides(2)were prepared by the reaction of 1-substituted pyrazolo[3,4-d]-oxazinone(1) with amines in benzene.The compound 2 was refluxed with excess LiAlH_4 in a mixture of THF and ether,one of the two carbamoyl groups in the molecule 2 was reduced selectively.As the results,1-substituted-5- benzylamino-4-pyrazolecarboxamides(3)were obtained.Compounds 3 reacted with Cl_2PPh-X,or P(NET_2)_3,producing the title compounds(4). The conditions of the reactions were studied.展开更多
A new three-arms-nine-chains discotic molecule has been synthesized,and the aggregation structure of the compound was measured by x-ray diffraction,infrared spectra,polarizing microscope,etc.From these evidences,the n...A new three-arms-nine-chains discotic molecule has been synthesized,and the aggregation structure of the compound was measured by x-ray diffraction,infrared spectra,polarizing microscope,etc.From these evidences,the new discotic liquid crystal is found to have the discotic lammelar phase.展开更多
Ointment-like poly(ortho esters) were synthesized from the reaction of 3,9-bis (methylene)-2,4,8,10-tetraoxaspiro[5.5]undecane with PEG-400,N,N-bis(2-hydroxyethyl)-n-hexadecylamine and N,N-bis(2-hydroxyethyl) palmitam...Ointment-like poly(ortho esters) were synthesized from the reaction of 3,9-bis (methylene)-2,4,8,10-tetraoxaspiro[5.5]undecane with PEG-400,N,N-bis(2-hydroxyethyl)-n-hexadecylamine and N,N-bis(2-hydroxyethyl) palmitamide respectively. The influence of the catalyst on the intrinsic viscosity of polymers was also studied.展开更多
The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are po...The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are potentially useful precursors for the synthesis of C-3 linked binuclear compounds.展开更多
The chlorination of O,O-dialkyl N,N-dialkyl thiophosphoramidates with phosphorus oxychloride proceeds with isomerization to give S-alkyl N,N-dialkyl thiophosphoramidochloridates,which react further with various nucleo...The chlorination of O,O-dialkyl N,N-dialkyl thiophosphoramidates with phosphorus oxychloride proceeds with isomerization to give S-alkyl N,N-dialkyl thiophosphoramidochloridates,which react further with various nucleophiles in the presence of base to give the title compounds.展开更多
An intramolecular nucleophilic substitution of carbon anion to cyclic sulfate was first employed in asymmetric synthesis of (+)-(3R, 4S, 5R, 7S)-neoclausenamide 1 which is a novel hepatoprotective lactam isolated from...An intramolecular nucleophilic substitution of carbon anion to cyclic sulfate was first employed in asymmetric synthesis of (+)-(3R, 4S, 5R, 7S)-neoclausenamide 1 which is a novel hepatoprotective lactam isolated from the dry leaves of Chinese folk medicine Clausena lansium (Lour) Skeel. The regioselectivity of beta-attack to this cyclic sulfate, just like its epoxide counterpart was attributed to the increased reactivity of beta-position by the phenyl group.展开更多
Three kinds of products have been separated from the reaction mixtures of 1,2-dihydro-2, 4-disubstituted-1,5-benzodiazepine with: CCI_2.Besides the addition products of: CCI_2 to C=N.the inserted products of: CCI_2 to...Three kinds of products have been separated from the reaction mixtures of 1,2-dihydro-2, 4-disubstituted-1,5-benzodiazepine with: CCI_2.Besides the addition products of: CCI_2 to C=N.the inserted products of: CCI_2 to N-H and C-H single bonds were obtained, too.展开更多
o-Carboxybenzaldehyde (1)and acetone gave the Claisen-Schmidt condensation product, which readily cyclizes on acidification to give 1-oxo-3-acetonyl-dihydrobenzo [c]furan(4)in 68% yield. Other methyl ketones behaved s...o-Carboxybenzaldehyde (1)and acetone gave the Claisen-Schmidt condensation product, which readily cyclizes on acidification to give 1-oxo-3-acetonyl-dihydrobenzo [c]furan(4)in 68% yield. Other methyl ketones behaved similarly.展开更多
Isobutyraldehyde was used as starting material via three steps: oxidation, chlorination and dehydro-chlorination to yield methacrylic acid. The total yield of methacrylic acid is 49.7%.
Sixteen new 1,6-disubstituted fulvenes have been prepared by acylation of cyclopentadienyl sodium and the result of preliminary pharmacological tests showed that several of them have antineoplastic activity.
A series of compounds,which are structurally analogous to scopolamine and also in accordance with the general formula of neuroleptic benzamides,were synthesized and tested for their potential antipsychotic activity.
文摘Using N-bromosuccinimide and pyridine as the oxidation system to dehydrogenate aryl substituted semicarbazide to form azo compounds is described for the first time in this paper. Nine azo compounds have been prepared in excellent yield under mild condition. This method only. needs simple instrument and short reaction time.
基金Project supported by National Natural Science Foundation of China(No.2870083)
文摘A new method to tetrahydro-β-carbolines(βCs) from tryptamine is described and the aromatization of THβCs to βCs by manganese dioxide is reported for the first time in this type of compounds.
文摘Nor-ketoagarofuran (1), one of the furanoids isolated from grnd Oil, has been Synthesed in a preprative scale in high yield from olefin 3 in 3 steps. Reaction of norketoagarofuran (1) with CH3MgI afforded 4 (2), an another naturallyoccurring tetrahydrofuran derivative.
文摘Arenesulfonyl chloride undergoes a facile one-pot coupling reaction with active halides assisted by zinc to give the corresponding sulfones in acceptable yields.
文摘This paper describes the direct oxidation of pyridines to pyridine-N-oxides by means of 30% H2O2 in aq media in the presence of Na2WO4.2H(2)O as catalyst instead of with per-acids or 30% H2O2 in acetic acid. Good yields were obtained.
文摘The reaction of two series of 2,3-dihydro-1,5-henzothiazepines Ⅰ with dichloro- carbene,gave azirino[2,1-d][1,5]benzothiazepines Ⅷ,azirino[2,1-e][1,6]benzothiazocines Ⅸ, pyrrolo[2,1-b][1,3]benzothiazoles Ⅹ,substituted-cyclopropanes Ⅺ and 2H-1,4-benzothiazin-2-ones Ⅻ.The structures of these products were confirmed by the analytical and spectral data.Compound Ⅷ and Ⅸ are two new ring systems.
文摘A new prenylated flavonol, maackiaflavonol, was isolated from the ethanol extract of the roots of Maackia tenuifolia. Its structure was elucidated as 7-hydrox-8-prenylflavonol by means of spectroscopic analysis (UV, IR, MS, NMR and 1H-1H COSY) and confirmed by total synthesis.
基金Project supported by National Natural Science Foundation of China.
文摘1-substituted-5-benzoylamino-4-pyrazolecarboxamides(2)were prepared by the reaction of 1-substituted pyrazolo[3,4-d]-oxazinone(1) with amines in benzene.The compound 2 was refluxed with excess LiAlH_4 in a mixture of THF and ether,one of the two carbamoyl groups in the molecule 2 was reduced selectively.As the results,1-substituted-5- benzylamino-4-pyrazolecarboxamides(3)were obtained.Compounds 3 reacted with Cl_2PPh-X,or P(NET_2)_3,producing the title compounds(4). The conditions of the reactions were studied.
文摘A new three-arms-nine-chains discotic molecule has been synthesized,and the aggregation structure of the compound was measured by x-ray diffraction,infrared spectra,polarizing microscope,etc.From these evidences,the new discotic liquid crystal is found to have the discotic lammelar phase.
文摘Ointment-like poly(ortho esters) were synthesized from the reaction of 3,9-bis (methylene)-2,4,8,10-tetraoxaspiro[5.5]undecane with PEG-400,N,N-bis(2-hydroxyethyl)-n-hexadecylamine and N,N-bis(2-hydroxyethyl) palmitamide respectively. The influence of the catalyst on the intrinsic viscosity of polymers was also studied.
文摘The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are potentially useful precursors for the synthesis of C-3 linked binuclear compounds.
文摘The chlorination of O,O-dialkyl N,N-dialkyl thiophosphoramidates with phosphorus oxychloride proceeds with isomerization to give S-alkyl N,N-dialkyl thiophosphoramidochloridates,which react further with various nucleophiles in the presence of base to give the title compounds.
文摘An intramolecular nucleophilic substitution of carbon anion to cyclic sulfate was first employed in asymmetric synthesis of (+)-(3R, 4S, 5R, 7S)-neoclausenamide 1 which is a novel hepatoprotective lactam isolated from the dry leaves of Chinese folk medicine Clausena lansium (Lour) Skeel. The regioselectivity of beta-attack to this cyclic sulfate, just like its epoxide counterpart was attributed to the increased reactivity of beta-position by the phenyl group.
文摘Three kinds of products have been separated from the reaction mixtures of 1,2-dihydro-2, 4-disubstituted-1,5-benzodiazepine with: CCI_2.Besides the addition products of: CCI_2 to C=N.the inserted products of: CCI_2 to N-H and C-H single bonds were obtained, too.
文摘o-Carboxybenzaldehyde (1)and acetone gave the Claisen-Schmidt condensation product, which readily cyclizes on acidification to give 1-oxo-3-acetonyl-dihydrobenzo [c]furan(4)in 68% yield. Other methyl ketones behaved similarly.
文摘Isobutyraldehyde was used as starting material via three steps: oxidation, chlorination and dehydro-chlorination to yield methacrylic acid. The total yield of methacrylic acid is 49.7%.
文摘Sixteen new 1,6-disubstituted fulvenes have been prepared by acylation of cyclopentadienyl sodium and the result of preliminary pharmacological tests showed that several of them have antineoplastic activity.
文摘A series of compounds,which are structurally analogous to scopolamine and also in accordance with the general formula of neuroleptic benzamides,were synthesized and tested for their potential antipsychotic activity.
