Efficient synthesis of 4（3H）-quinazolinones using a soluble polymeric support

4（3H）-Quinazolinones have been synthesized from poly（ethylene glycol） （PEG） supported aza-Wittig reaction. 2-Dialkylamino- 4（3H）-quinazolinones 6 were synthesized efficiently by reaction of secondary amine with PEG-supported carbodiimides 4, which were obtained from aza-Wittig reaction of PEG-supported iminophosphoranes 3 with isocyanates.     

Synthesis and Crystal Structure of a New Quinazolinone Compound 2,3-Dihydro-2-（2-hydroxyphenyl）-3-phenyl-quinazolin-4（1H）-one

A new quinazolinone compound 2,3-dihydro-2-(2-hydroxyphenyl)-3-phenylquinazolin-4(IH)-one 3 ([C2oH16O2N2]-C2H5OH, Mr = 362.42) and compound 2-(2-hydroxybenzylidene-amino)-N-phenyl-benzamide 2 (C2oH16O2N2, Mr = 316.34) were prepared from a precursor of 2-amino-N-phenyl-benzamide 1 (C13H12ON2, Mr = 212.25). Compound 3 was characterized by single-crystal X-ray diffraction analysis. The crystal belongs to orthorhombic,space group Pbca with a = 1.2889(11), b = 1.6170(14), c = 1.7729(15) nm, V= 3.695(6) nm^3, Z= 8, F(000) = 1536, Mr = 362.42, Dc = 1.303 g/cm^3, μ(MoKa) = 0.087 mm^-1, R = 0.0447 and wR= 0.0879. The crystal structure analysis indicates that the title compound has a two-dimensional network structure formed by hydrogen bonds and electrostatic interactions.     

Synthesis, Crystal Structure and Antibacterial Activities of 3-[（2-Hydroxy-4-diethylamino-phenyl）methylenehydrazinocarbonyl]-4-hydroxy-6-methyl-2（1H）-pyridinones

1 INTRODUCTION Recently, compounds containing pyrazole, imida- zole, triazole (including benzotriazole), pyridine, tetrazole and indole have attracted much interest because of their fungicidal activity, plant-growth regulating activity and antibacterial activity[1～3]. Schiff bases also constitute a good type of biolo- gically active substructures[4～7]. Studies of pyri- dine Schiff base-type fungicides have been repor- ted[8]. However, some structures of pyridine com- pounds containing h…     

An Efficient Synthesis of Highly Optically Active 4-Substituted-2（5H）-furanones from Chiral 3-Bromo-2（5H）-furanone

Highly optically active 4-substituted-2(5H)-furanones 6a-6j were obtained in good yields with de≥98% by the tandem Michael addition/elimination reaction of chiral 3-bromo-2(SH)-furanone (4a), which was conveniently prepared starting from 2-furaldehyde under mild conditions. The products were identified on the basis of their satisfactory elemental analysis and spectroscopic data of IR, UV, ^1H NMR, ^13C NMR and mass spectra. The stereochemistry and absolute configuration of this type of compounds were established by the X-ray crystallographic study. The reaction provided a short and efficient synthesis of the interesting highly optically active 4-subsdtuted-2(5H)-furanones containing an active pyrimidine and a purine base group.     

A Selective Synthesis of 2-Alkylamino-5, 6, 7, 8-tetrahydrobenzothieno[2, 3-d]pyrimidin-4（3H）-ones

2-Alkylamino-5, 6, 7, 8-tetrahydrobenzothieno [2,3-d] pyrimidin-4(3H)-ones 7 were synthesized by a new selective synthetic method, which includes aza-Wittig reaction of iminophosphorane 4 with aromatic isocynate to give carbodiimide 5 and subsequent reaction of 5 with various aliphatic primary amine in the presence of EtO^-Na^ .     

Synthesis and Crystal Structure of 4-（4-Bromophenyl）- 3,4-dihydro-6-methyl quinolin-2（1H）-one

The title compound (C16H14BrNO) has been synthesized by the reaction of p-tolylamine, Meldrum’s acid and 4-bromo-benzaldehyde, and its structure was characterized by IR, 1H NMR and X-ray single-crystal diffraction. The crystal belongs to monoclinic, space group P21/n with a = 7.6850(11), b = 8.3004(11), c = 21.301(3) , β = 95.110(2)°, V = 1353.4(3) 3, Mr = 316.19, Z = 4, Dc = 1.552 g/cm3, μ(MoKα) = 3.028 mm-1, F(000) = 640, the final R = 0.0345 and wR = 0.0768. X-ray analysis reveals that the atoms of C(1), C(2), C(3), C(4), C(5) and N(1) form a six-membered ring of boat conformation.     

H-Y-zeolites induced heterocyclization： Highly efficient synthesis of substituted-quinazolin-4（3H）ones under microwave irradiation

A highly efficient synthesis of 2-amino-N-substituted-benzamides was performed by the condensation of isatoic anhydride with several amines in solvent-free conditions under microwave irradiation. H-Y-zeolites induced heterocyclization of these products with ortho-esters under similar conditions afforded the relevant substituted-quinazolin-4(3H)ones in high yields.     

Synthesis of 4-(4-Methylsulfonylphenyl)-3-phenyl-2(3H)-thiazole Thione Derivatives as New Potential COX-2 Inhibitors

Synthesis of novel 4-（4-methylsulfonylphenyl）-3-phenyl-2（3H）-thiazole thione derivatives with functionalized diarylheterocycle pharmacophore as potential COX-2 inhibitors was described. The title compounds were synthesized by cyclocondensation of corresponding dithiocarbamate and 2-bromo-1-（4-methylsulfonylphenyl）ethanone, followed by dehydration with H2SO4. All of the target compounds were characterized by ^1H NMR, IR and mass spectral data.     

Synthesis of Novel Nucleoside Analog （3R）-2,3-Dideoxy-3-（N-hydroxy-N-methylamino）-L-arabinofuranosyl Uracil

The synthesis of novel nucleoside analog (3R)-2,3-dideoxy-3-(N-hydroxy-N-methylamino)-L-arabinofuranosyl uracil was studied. A twelve-step synthetic route, started from L-ascorbic acid, was designed, and the final product was obtained in 20.8% yield.     

Synthesis and Structure of [Er4（μ3—OH）4（Hpro）4（Pro）2（H2O）7]（ClO4）6.7H2O

1 INTRODUCTION The design and synthesis of polynuclear com- plexes have attracted chemists?attention in the contemporary chemistry, since their clusters maybe lead to novel materials with magnetic, optical, electronic and catalytic properties of the constituent metals[1～3]. It is also prevalently interesting to synthesize high-nuclearity metal complexes for their nanoscopic dimensions[3, 4]. Spectroscopic properties of the lanthanides are widely used in the study of biological systems. …     

Synthesis and Crystal Structure of DinuclearCadmium Complex [Cd2（phen）4（fca）2]（ClO4）2-（H2O）2

1 INTRODUCTION During the search of molecule-based materials with interesting properties such as catalysis, cla- thration etc., much attention has been focused on the synthesis of one-, two- and three-dimensional extended solids involving cadmium[1], as its d10 configuration permits a wide variety of geometries and coordination numbers. Rigid bridged ligands such as carboxylate groups are frequently used to construct these materials. Therefore, the coordi- nation chemistry of Cd(Ⅱ) ca…     

Synthesis and Structure Characterization of N-Phenyl-（2S）-hydroxy-3-[（2-hydroxybenzylidene）amino]propionamide

1 INTRODUCTION Schiff bases can be conveniently prepared from the corresponding aldehyde and primary amine, which, as multidentate ligands, have already received great attention. Many metal complexes of this kind of ligands have been used successfully in various re- actions, such as Diels-Alder and hetero-Diels-Alder reactions[1], kinetic resolution of racemic epoxides[2], and Nozaki-Hiyama-Kishi (NHK) reaction[3]. Recen- tly Berkessel et al. have reported that the Cr- complex of sal…     

Crystal Structure and DFT Studies of a Triazole Derivative： 4- （ 2-Hydrobenzylideneamino ） -3- （ 1,2,4-triazol-4-ylmethyl） 1H-1, 2,4-triazole-5 （4H） -thione

A novel triazole derivative 4-(2-hydrobenzylideneamino)-3-(1,2,4-triazol-4-ylmethyl)-1H-1,2,4-triazole-5(4H)-thione(1) was synthesized and characterized using elemental analysis, FTIR, and 1H NMR, and its crystal structure was determined via X-ray single crystal diffraction analysis. Crystal data: monoclinic, P2(1)/c, a=0.83335(9) nm, b=1.49777(16) nm, c=1.14724(12) nm, β =107.990(2)°, D=1.470 Mg/m3, and Z=4. The geometries and the vibrational frequencies were determined using the density functional theory(DFT) method at the B3LYP/ 6-31G level. To demonstrate the accuracy of the reaction route of compound 1, one of the important intermediates was also tested using the same method. The structural parameters of the two compounds calculated using the DFT study are close to those of the crystals, and the harmonic vibrations of the two compounds computed via the DFT method are in good agreement with those in the observed IR spectral data. The thermodynamic properties of the title compound were calculated, and the compound shows a good structural stability at normal temperature. The test results of biological activities show that it has a certain bactericidal ability.     

Synthesis and Structure of [Cu（OH）2（H2O）2（4—C5H4N—COOH）2]

1 INTRODUCTION Supramolecular chemistry and crystal engineering of coordination compounds have attracted considerable interests nowadays owing to the fascinating structural diversity and potential applications as functional materials[1,2]. Generally, architectures of supramolecules are formed through hydrogen bonds, ?- ?stacking interaction or other weak interactions between the molecules. Recently, many supramolecular compounds containing silver(I) and copper(II) species have been re-…     

A Rapid Parallel Synthesis of 2-Dialkylamino-4(3H)-quinazolines

Many 4(3H)-quinazolinones possess biological and pharmaceutical activities. For example, some of them exhibited good antiinflammatory and noncompetitive AMPA receptor antagonistical activities1-3, whereas others exhibited good anticancer and antiviral activities4-6. Among them, 2-amino-4(3H)-quinazolinones were found to show significant fungicidal activities or used as potential potassium channel openers7-9. Recently, combinatorial synthesis of libraries containing small organic molecules …     

A Convenient Synthesis of 6,8-Dimethoxy-3-[（2-（4-methoxyphenyl）ethyl）isocoumarin

6,8-Dimethoxy-3-[2-（4-methoxyphenyl）ethyl]isocoumarin was synthesized by condensation of 5,7-dimethoxyhompophthalic acid with 3-（4-methoxyphenyl）propanoyl chloride. The structure of the synthesized compound was confirmed by its mass spectrometric studies. The synthesized compound serves as a model for synthesis of DL-agrimonolide.     

A Novel Synthesis of Bis-（1,2,4-triazolyl）-3-disulfides

Manganese triacetate was introduced as a new reagent for radical cyclization of substituted aminothioureas. Bis-（1,2,4-triazolyl）-3-disulfides were generated in 10 min under microwave irradiation.     

Synthesis and Crystal Structure of a Novel Three-dimensional Supramolecular Compound [（AgI3）（4-HBPFA）2（H2O）]

1 INTRODUCTION In recent years, the rational design and synthesisof metal-directed supramolecular frameworks throughintermolecular hydrogen bonds, π-π stacking interac-tion or other weak interactions have received muchattention because of their interesting molecular topo-logies and various potential applications in catalysis,superconductor, magnetism, nonlinear optics, sen-sors and molecular recognition[1～4]. On the otherhand, the attachment of mono- or polypyridyl frag-ments to a ferr…