Diels-alder reactions of 2- and 3-vinyl-1-(phenylsulfonyl)pyrroles

Regioselectively produced 2- and 3-acetyl-1-(phenylsulfonyl)pyrroles can be reduced to the corresponding alcohols and subsequently dehydrated to afford N-protected vinylpyrroles. These remarkably stable vinylpyrroles can then serve as heterodienes in [4 + 2] cycloaddition reactions with electron deficient dienophiles to afford tetrahydroindole derivatives.     

Synthesis of 4″-benzyloxyimino-4″-deoxyavermectin Bla derivatives

Six new 4″-benzyloxyimino-4″-deoxyavermectin Bla derivatives were synthesized from avermectin Bla by the selective protection of C-5-hydroxy group,oxidation of C-4″-hydroxy group,and deprotection followed by reaction with O-substituted hydroxylamine hydrochlorides.Their structures were confirmed by IR,~1H NMR,~(13)C NMR and MS.Insecticidal activities of the derivatives against Phopalosiphum pseudobrassicae,Spodoptera exigua and Pluteua xylosteua were evaluated.     

Synthesis and Crystal Structure of a Novel Compound of （C2N2H8O2） H6V10O28

A novel vanadate decamer, involving all vanadium atoms present in +5 oxidation and one formhydroxamic acid dimer cation readical, has been synthesized. The single-crystal X-ray diffraction shows that the orange crystal is formed in the triclinic system, space group Pi, a = 8. 4960 (17), b = 10.447 (2), c = 11.299 (2) A, α= 68. 82 (3)°,β= 87.35 (3)°, γ = 66.97(3)°. V = 855. 3(3) A3, Z = 8, R1 = 0. 0857, wR2=0. 2551. X-ray crystallographic and packing in superlattice studies showed that the crystal structure was constructed by electrostatic attraction of O-H…O hydrogen bonds between formhydroxamic acid dimer cation and decavanadate polyanion. Formhydroxamic acid dimer is got through controlling the condition of the reaction using formhydroxamic acid.     

Palladium-catalyzed amination of aryl bromides with hindered N-alkyl-substituted anilines using a palladium(I) tri-tert-butylphosphine bromide dimer

An efficient palladium-catalyzed amination of aromatic bromides with hindered N-alkyl-substituted anilines is described, either using the combination of Pd(OAc)(2) and P(t-Bu)(3) or a palladium(I) tri-tert-butylphosphine bromide dimer, [Pd(mu-Br)(t-Bu(3)P)](2), a new, commercially available, and easily handled catalyst.     

Immunoassay of P-glycoprotein on single cell by capillary electrophoresis with laser induced fluorescence detection

The cellular mechanism based on P-glycoprotein (PGP) for its drug pump function has become very important in multidrug resistance (MDR) research. A method has been established to characterize PGP on single K562 cell by coupling capillary electrophoresis with laser induced fluorescence detection. A permeable intact cell after the immunoassay binding with fluorescence labeling antibody was injected into the capillary and directly separated without lysis. It was found that once 5-10 optional cells were detected in batch, the PGP amount on this cell line could be outlined and calculated clearly. The PGP amount on K562 MDR cell line is 3.88 times higher than that on K562 sensitive cell line. These two cell lines with immunoassay binding were also analyzed by injection of multi-cells in order to improve the throughput. A resistance factor so called multidrug resistance multiple (MRM) was introduced to evaluate the MDR difference between cell lines. The MRM values of the cell line K562 measured by single cell analysis are well correlated with those by flow cytometry, which also prove the validity of our method in single cell analysis for the possibility of cancer diagnosis, pharmacokinetics and drug screening in future.     

Efficient synthesis of p-bis-(chlorodifluoromethyl)benzene

Selective, high yield partial fluorination of p-bis-(trichloromethyl)benzene to p-bis-(chlorodifluoromethyl)benzene has been accomplished by warming a slurry of the p-bis-(trichloromethyl)benzene in anhydrous HF which also contains a small quantity of inert solvent, such as 1,2-dichloroethane.     

Reduction of 4-nitrophenol catalyzed by nitroreductase

The reduction of 4-nitrophenol catalyzed by nitroreductase in the presence of NADH was investigated in this paper.4-Amino- phenol and 4-bydroxylamino-phenol were found in the reductive products.The relationship between reaction time and the reductive ratio were studied.The similar reducing ratios of 4-nitrophenol were obtained under aerobic and anaerobic conditions.The results indicated that an oxygen-insensitive reaction was proceeded in the reduction of 4-nitrophenol and nitroreductase was an oxygen- insensitive enzyme.The reductive products of 4-nitrophenol were determined by HPLC and MS.     

A Novel Plasticizer for the Preparation of Thermoplastic Starch

TPS was a biodegradable material based on starch. Starch was an inexpensive and natural renewable polysaccharide, which was widely investigated as the substitute of petroleum-derived plastics. Native starch commonly existed in granule structure with about…     

Chemical Constituents from Cynoglossum gansuense

Two new alkaloids, i.e., (2,3‐dihydro‐1‐oxo‐1H‐pyrrolo[1,2‐a]pyrrol‐7‐yl)methyl (2S*,3S*)‐3‐[(β‐D ‐glucopyranosyl)oxy]‐2‐hydroxy‐2‐(1‐methylethyl)butanoate ( 1 ) and 1,2‐dihydro‐8‐methoxy‐2‐oxoquinoline‐4‐carboxylic acid ( 2 ), were isolated from the alcoholic extract of the whole plant of Cynoglossum gansuense, together with twelve known compounds Their structures were characterized by means of spectroscopic methods, especially by ¹H‐, ¹³C‐, and 2D‐NMR, as well as by HR‐MS experiments and comparison with literature data.