1,2-O-Isopropylidene-5-O-p-toluenesulfonyl-α-D-erythro-pentofuranos-3-ulose 1 was treated with thiourea and aminothiourea to give a D-ribose derivative 2 bearing a 2-amino 1,3-thiazine ring and a thiosemicarbazone de...1,2-O-Isopropylidene-5-O-p-toluenesulfonyl-α-D-erythro-pentofuranos-3-ulose 1 was treated with thiourea and aminothiourea to give a D-ribose derivative 2 bearing a 2-amino 1,3-thiazine ring and a thiosemicarbazone derivative 5, respectively. 2 was acylated with Ac20 and propandioic acid to afford two acylation derivatives 3 and 4, respectively. Reduction of 5 with NaBH4 in methanol produced a hydrothiosemicarbazone derivative 6. The absolute configuration of 2 was confirmed by X-ray crystallographic analysis. The structures of all products were elucidated by IR, NMR and HRMS spectra.展开更多
Thiazine sugar derivative 2 was synthesized and characterized by IR, NMR and H RMS, and its crystal structure was determined by X-ray diffraction analysis. The crystal is of monoclinic system （C16H24N2O8S2, Mr = 436...Thiazine sugar derivative 2 was synthesized and characterized by IR, NMR and H RMS, and its crystal structure was determined by X-ray diffraction analysis. The crystal is of monoclinic system （C16H24N2O8S2, Mr = 436.49） with space group P21, a = 10.311（2）, b = 9.1198（18）, c = 11.623（2）A, β = 109.47（3）°, V= 1030.4（4）A^3, Z= 2, Dc = 1.407 g/cm^3, F（000）= 460, μ= 0.303 mm^-1, the final R = 0.0437 and wR = 0.0561 for 1954 observed reflections （I 〉 2σ（I））. Nine hydrogen bonds were found. The absolute configuration of this molecule was confirmed by comparison with the original material.展开更多
A series of novel multithioether derivatives were synthesized by the combination of thiazoline and thiazine with dibro- mides and their structures were characterized by IR, 1H NMR, MS and elemental analysis. The synth...A series of novel multithioether derivatives were synthesized by the combination of thiazoline and thiazine with dibro- mides and their structures were characterized by IR, 1H NMR, MS and elemental analysis. The synthesized derivatives were tested for antitumor activity.展开更多
An efficient synthesis of thiazines from the three component reactions between dialkyl acetylenedicarboxylates, arylisothio- cyanates and N-nucleophiles at room temperature in water as the solvent is described.
Methylene blue(MB) is commonly used in aquaculture as a fungicide and antidotes. This study was designed to explore the pharmacokinetics of MB in Japanese eel(Anguilla Japonica) immersed in 10 mg L^-1 and 20 mg L^-1 M...Methylene blue(MB) is commonly used in aquaculture as a fungicide and antidotes. This study was designed to explore the pharmacokinetics of MB in Japanese eel(Anguilla Japonica) immersed in 10 mg L^-1 and 20 mg L^-1 MB for 0.5 h. The concentrations of MB and its derivatives in the blood, liver, kidney, skin and muscle were determined by HPLC after immersion. The results showed that the changes of drug concentrations in Japanese eel were basically the same in different dose groups, showing a general trend of increasing at first and then decreasing, but the peak time was slightly different. The peak concentration of the drug was positively correlated with the dose level. The peak concentrations of MB in MB(20 mg L^-1) group, MB, azure A and azure B in the tissues of Japanese eel were significantly higher than those in MB(10 mg L^-1) group. Moreover, MB, azure A and azure B remained for a long time and could still be detected at 64 days, and azure C was not detected in tissues.展开更多
基金the National Natural Science Foundation of China(No.20472075)for financial support of this work.
文摘1,2-O-Isopropylidene-5-O-p-toluenesulfonyl-α-D-erythro-pentofuranos-3-ulose 1 was treated with thiourea and aminothiourea to give a D-ribose derivative 2 bearing a 2-amino 1,3-thiazine ring and a thiosemicarbazone derivative 5, respectively. 2 was acylated with Ac20 and propandioic acid to afford two acylation derivatives 3 and 4, respectively. Reduction of 5 with NaBH4 in methanol produced a hydrothiosemicarbazone derivative 6. The absolute configuration of 2 was confirmed by X-ray crystallographic analysis. The structures of all products were elucidated by IR, NMR and HRMS spectra.
文摘Thiazine sugar derivative 2 was synthesized and characterized by IR, NMR and H RMS, and its crystal structure was determined by X-ray diffraction analysis. The crystal is of monoclinic system （C16H24N2O8S2, Mr = 436.49） with space group P21, a = 10.311（2）, b = 9.1198（18）, c = 11.623（2）A, β = 109.47（3）°, V= 1030.4（4）A^3, Z= 2, Dc = 1.407 g/cm^3, F（000）= 460, μ= 0.303 mm^-1, the final R = 0.0437 and wR = 0.0561 for 1954 observed reflections （I 〉 2σ（I））. Nine hydrogen bonds were found. The absolute configuration of this molecule was confirmed by comparison with the original material.
文摘A series of novel multithioether derivatives were synthesized by the combination of thiazoline and thiazine with dibro- mides and their structures were characterized by IR, 1H NMR, MS and elemental analysis. The synthesized derivatives were tested for antitumor activity.
文摘An efficient synthesis of thiazines from the three component reactions between dialkyl acetylenedicarboxylates, arylisothio- cyanates and N-nucleophiles at room temperature in water as the solvent is described.
基金supported by the National Key R&D Program of China (No.2019YFD0900102)the Science and Technology Commission of Shanghai Municipality (Nos.17050502100 and 18391901500)+1 种基金the National Natural Resources Platform of ChinaKnowledge Service Platform of Shanghai Ocean University。
文摘Methylene blue(MB) is commonly used in aquaculture as a fungicide and antidotes. This study was designed to explore the pharmacokinetics of MB in Japanese eel(Anguilla Japonica) immersed in 10 mg L^-1 and 20 mg L^-1 MB for 0.5 h. The concentrations of MB and its derivatives in the blood, liver, kidney, skin and muscle were determined by HPLC after immersion. The results showed that the changes of drug concentrations in Japanese eel were basically the same in different dose groups, showing a general trend of increasing at first and then decreasing, but the peak time was slightly different. The peak concentration of the drug was positively correlated with the dose level. The peak concentrations of MB in MB(20 mg L^-1) group, MB, azure A and azure B in the tissues of Japanese eel were significantly higher than those in MB(10 mg L^-1) group. Moreover, MB, azure A and azure B remained for a long time and could still be detected at 64 days, and azure C was not detected in tissues.
