A Solid Phase Synthesis of Chalcones by Claisen-Schmidt Condensations

In order to accelerate the development of relatively inexpensive antimalarials that are effective against chloroquine-resistant strains of Plasmodium falciparum, a methodology for the solid phase synthesis of chalcone (1, 3-diphenyl-2-propen-1-one) analogues in reasonably high yields has been developed.

A Facile Solid-phase Synthesis of 3-Carboxycoumarins

Carboxycoumsrins were synthesized via the solid phase synthesis conviently. The resin bound cyclic malonic ester reacted with o-methoxy or o-hydroxybenzaldehydes. Then cyclization was processed under H2SO4 to afford the products in excellent purities and yields.

APPLICATION OF THE SULFONATE ESTER GROUP AS A LINKER FOR SOLID PHASE ORGANIC SYNTHESIS

A use of Sulfonate ester as a linker in synthesis of (-aminoalkanols was reported. Diols were tethered onto polystyryl sulfonyl chloride resin, yielding sulfonate resins (2). After cleaved by diethyl amine, diisopropylamine and propylamine respectively, three (-aminoalkanols were obtained.

Solid Phase Synthesis of 4(1H)Quinolones from Resin-Bound Cyclic Malonic Ester

The solid phase synthesis of 4 (1H) quinolones has been reported.

Solid Phase Synthesis of β-Carbolines

Synthesis of β-carbolines on solid phase using TCCA as the key reagent is developed.

Solid Phase Synthesis of 4H-Pyrimido[2,1-b] Benzothiazol-4-ones from Resin-Bound Cyclic Malonic Ester

The solid phase synthesis of 4H-pyrimido[2,1-b] benzothiazol-4-ones has been reported.

Solid-phase Synthesis of-Haloaldehydes from Polymer-supported 4-(Phenylseleno)morpholine

Polystyrene-supported 4-(phenylseleno)morpholine was synthesized and could be used as an efficient ?selenenylating agent for saturated aldehydes. ?Haloaldehydes were prepared by reaction of polystyrene-supported ?selenoaldehydes with bromine or sulfuryl chloride in good yield and high purity.

Solid-Phase Stereoselective Synthesis of (E)-1, 2-Disubstituted Ethenes from Polymer-Sopported a-Selenoaldehydes

Reaction of polymer-supported a-selenoaldehydes with Grignard reagents afforded polymer-bound B-hydroxyalkyl selenides, which treated with thionyl chloride and triethylamine leading to (E)-1, 2-disubstituted ethenes in good yield.

Solid Phase Peptide Synthesis of Fusukang for AIDS

A 36-residue peptide is designed to cure acquired immunodeficiency syndrome(AIDS), and is synthesized by the manual solid phase peptide synthesis technique. Different reaction conditions of the synthesis process were discussed. Stirring efficiency of mechanics and nitrogen was compared. The mechanical method displays a predominant performance. Although the coupling efficiencies of diisopropylcarbodiimide(DIC) and dicyclohexylcarbodiimide(DCC) are virtually identical, DIC offers several advantages over DCC in practice due to different physical characters. Wash conditions after deprotection and coupling were investigated to monitor washing efficiency. 0.369 2 g crude peptide was obtained.

Traceless solid-phase synthesis of 3-substituted isoxazoles from polystyrene-supported vinyl selenide

A novel facile procedure for traceless solid-phase synthesis of 3-substituted isoxazoles in good yields and with excellent purities using polymer-supported vinyl selenide has been developed.

Solid-Phase Synthesis of Acrylamide Using Polymer-Supported β-Selenopropionic Acid

A novel polystyrene-supported ?selenopropionic acid has been developed and applied to facile synthesis of acrylamides.

Solid-phase synthesis of (Z)-allyl iodides from 3-acetoxy-2-methylene-alkanoates with recyclable polymer-supported selenium bromide

Reaction of polystyrene-supported lithium selenide with 3-acetoxy-2-methylene-alkanoates afforded the corresponding allyl selenide resins and subsequent cleavage from the polymer by treating with methyl iodide to furnish （Z）-allyl iodides in good yields and high purities. The polymeric selenium reagent can be regenerated and reused. So it is a environmentally benign reagent.

Solid-phase Synthesis of Unsaturated β-Dicarbonyl Compounds from Polymer-supported 4-(Phenylseleno)morpholine

The solid-phase synthesis of unsaturated ?dicarbonyl compounds has been reported.

SOLID PHASE SYNTHESIS OF ISOXAZOLINES

The solid-phase synthesis of isoxazolines on 2-polystyrylsulfonamidoethanol resin is reported. 2-Polystyrylsulfonamidoethanol resin 1 was reacted with acryloyl chloride to afford 2-polystyrylsulfonylamidoethyl acrylate resin 2, which was further reacted with brominated aldoximes by [3+2] cycloaddition to give isoxazoline resin 4. Resin 4 was treated with aqueous 6 mol/L HCl solution to obtain isoxazolines in good yield and purity.

Structure Based Library Approach to Photosynthesis Inhibitors:The Solid Phase Synthesis of Hydro-Uracils and Thiouracils

A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thioureas) 4 by treatment with isocyanates (isothiocyanates). Preparation of the hydro-uracils and thiouracils 5 is achieved by acidic cyclization-cleavage from the resin. The synthesis is designed to be amenable for structure based library approach to photosystem II D1 protein inhibitors.

Pyrolysis of single carbon sources in SBA-15: A recyclable solid phase synthesis to obtain uniform carbon dots with tunable luminescence

Most of carbon dots(CDs) are synthesized in solutions, but the extensive use of solvents produces too much waste, needs complex purification and results in low yield. Particularly for the popular hydrothermal/solvothermal syntheses, safety issues hinder the large-scale production of CDs. Solid phase synthesis in air seems perfect to solve the above problems once for all, but nanoparticle growth in solid phase is always difficult to control. Here we suggest a new method to synthesize CDs in SBA-15 template, just by heating single carbon sources in air. Employing single carbon sources is important, which ensures both homogeneity of the nucleation and uniformity of the nanoparticle growth. The pores confinement of SBA-15 guarantees the uniform sizes of CDs, while the catalytic effect of SBA-15 accelerates the carbonization process of precursors. The products are easily extracted from the template by ethanol, and then the template can be recycled for the next synthesis after calcination. Various CDs are synthesized in this way by using different carbon sources and SBA-15 templates with different pore diameters, respectively. The results show that, the fluorescence properties of these CDs are determined by their composition and surface states, but not the particle sizes. This work opens a new avenue to synthesize uniform CDs in solid phase with high yield, low cost and tunable luminescence.

Synthesis of nanosize MnO_2 and its performence

Sol sol gel method and solid phase redox reaction were respectively applied in preparation of Nanosize MnO 2 powders. The experiments showed that only Mn 2O 3 could be obtained from ignition of Mn(Ⅱ) in the muffle furnace in air, and Mn 2O 3 had to be disproportionated in acids to gain MnO 2. The analysis of XRD and TEM technique revealed that the diameters of nanosize MnO 2 obtained by sol gel method was 35～45 nm and the x in MnO x was 1 9; the particle size of MnO 2 produced from solid phase redox reaction was 10～20 nm and the x in MnO x equaled 1 94. The test results have proved that the discharge property of alkaline manganese battery could be improved by nanosize MnO 2.

Study on Chemical Synthesis and Insecticidal Activity of Peptideκ-CTx-btg02

[Objectives]This study was conducted to investigate the chemical synthesis of peptideκ-CTx-btg02.[Methods]Linear peptideκ-CTx-btg02 was synthesized by solid phase peptide synthesis(SPPS).After oxidation and folding of the linear peptide,mass spectrometry identification and high performance liquid chromatography(HPLC)purification were performed.Then,the MTT method and insect injection method were applied to study its insecticidal activity.[Results]The peptideκ-CTx-btg02 was successfully synthesized by the SPPS method,and identified for the formation of disulfide bonds by mass spectrometry identification,and the purity after HPLC separation was greater than 95%.The MTT experiment showed that the peptideκ-CTx-btg02 could inhibit the growth of insect cells sf9,with a half effective dose of 0.13 nM.The insect injection experiment showed that the peptideκ-CTx-btg02 could effectively kill Tenebrio molitor,with a half lethal dose of 15.6 nM.The results of the electrophysiological experiment showed that 10μM peptideκ-CTx-btg02 had no blocking activity on murine acetylcholineα2β3 andα3β4.Therefore,the peptideκ-CTx-btg02 had a good inhibitory effect on the growth of insect cells,highly effective insecticidal activity and weak mammalian toxicity.[Conclusions]This study lays a foundation for the development of new,safe and efficient peptide biological insecticides.

Synthesis of Peptoid Nucleic Acid with Thymine as Nucleic Base

The synthesis of peptoid nucleic acid bearing thymine as nucleobase has been achieved. This modified oligonucleotide showed good hybridization with DNA.

Polystyrene-supported Selenomethyl-sulfonates: Efficient Reagents for Stereocontrolled Synthesis of Substituted Vinyl Sulfones

Polystyrene-supported selenomethyl-sulfonates have been prepared. These novel reagents were treated with LDA to produce selenium stabilized carbanions, which reacted with alkyl halide and epoxides, followed by selenoxide syn-elimination, to give E-vinyl sulfones and -hydroxy-substituted-E-vinyl sulfones respectively.