Synthesis of a highly hydrophobic cyclic decapeptide by solid-phase synthesis of linear peptide and cyclization in solution

A general method was described to synthesize a highly hydrophobic cyclic peptide,cyclo[LWLWLWLWLQ]where underlines indicate D-configuration of the amino acid,by a two-step solid-phase/solution synthesis strategy.The linear decapeptide was assembled by standard Boc chemistry on solid-phase and subsequently cyclized in solution with high efficiency and reproducibility. In subsequent purification by semi-preparative HPLC,50%(v/v) DMF/H_2O was employed as the solvent to overcome the difficulty of solubilization...

Solid-phase synthesis of Cu2MoS4 nanoparticles for degradation of methyl blue under a halogen-tungsten lamp

The Cu_2MoS_4 nanoparticles were prepared using a relatively simple and convenient solid-phase process, which was applied for the first time. The crystalline structure, morphology, and optical properties of Cu_2MoS_4 nanoparticles were characterized using X-ray diffraction, X-ray photoelectron spectroscopy, field emission scanning electron microscopy, and UV-vis spectrophotometry. Cu_2MoS_4 nanoparticles having a band gap of 1.66 eV exhibits good photocatalytic activity in the degradation of methylene blue, which indicates that this simple process may be critical to facilitate the cheap production of photocatalysts.

Solid-phase Synthesis of PNA Monomer by Ugi Four-component Condensation Reaction

Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was tested by solid-phase synthesis. The Fmoc protected PNA monomer was build up with thymin-1-yl acetic acid, 3-methylbutyl aldehyde, Fmoc protected aminoethyl isocyanide and Gly-Wang resin.

Scalable solid-phase synthesis of defect-rich graphene for oxygen reduction electrocatalysis

Defect-engineered carbon materials have been emerged as promising electrocatalysts for oxygen reduction reaction(ORR)in metal-air batteries.Developing a facile strategy for the preparation of highly active nanocarbon electrocatalysts remains challenging.Herein,a low-cost and simple route is developed to synthesize defective graphene by pyrolyzing the mixture of glucose and carbon nitride.Molecular dynamics simulations reveal that the graphene formation is ascribed to two-dimensional layered feature of carbon nitride,and high compatibility of carbon nitride/glucose systems.Structural measurements suggest that the graphene possesses rich edge and topological defects.The graphene catalyst exhibits higher power density than commercial Pt/C catalyst in a primary Zn-air battery.Combining experimental results and theoretical thermodynamic analysis,it is identified that graphitic nitrogen-modified topological defects at carbon framework edges are responsible for the decent ORR performance.The strategy presented in this work can be can be scaled up readily to fabricate defective carbon materials.

Solid-phase Synthesis of Acyl-plasminogen-Streptokinase Activator Composite(APSAC) and Its Thrombolytic Properties

The dialysis method has been traditionally used for the conversion of native human plasminogen(Glu-Hpg) to lys-plasminogen(Lys-Hpg). Here is described a solid-phase synthesis method for the preparation of an acyl-plasminogen-streptokinase activator complex(APSAC) from Lys-Hpg, streptokinase(SK) and chemical modification (agent(4-amidinophenyl-4′-aminobenzoate hydrochloride)) with the L-lysine-Sepharose 4B Column as the carrier. The new method significantly increases the product yield and purity over the liquid-phase methods. The APSAC prepared with the new method exhibits a significant thrombolytic effect with a long half-life of about 8.8 h in rabbits.

Use of Magic Angle Spinning ~1H NMR Spectroscopy to Monitor Reactions in Solid-Phase Synthesis

Proton NMR-spectra of Wang resin bound compounds were obtained using the magic angle spinning 1HNMR technique with standard equipment. It was possible to analyse the spectra to evaluate their utility in solid-phase chernistry. A typical example was presented, which could directly monitor solid-phase reactions

Solid-Phase Enzymatic Peptide Synthesis to Produce an Antioxidant Dipeptide

Peptide bond synthesis is favorable to the production of bioactive small peptides. However, the abuse of toxic reagents remains an issue for chemical synthesis method, whereas the low product yield and purity limit the widespread use of enzymatic method. In this study, a new solid-phase enzymatic peptide synthesis(SPEPS) strategy was developed to produce an antioxidant tyrosine-alanine dipeptide(Tyr-Ala) by using recombinant carboxypeptidase Y(CPY) as the catalyst. The general SPEPS procedure involves three steps. First, the N-protected acyl donor was covalently attached to solid resin. Second,the peptide bond was condensed between the acyl donor and the nucleophile under the catalysis of CPY. Finally, one-step cleavage was performed to remove the protecting group and cleave the peptides from solid resin. Upon the optimization of reaction conditions, 77.92%(±2.723%) yield of Tyr-Ala with high product purity of 90.971%(±2.695%) was obtained.In addition, the antioxidant activity of Tyr-Ala was determined by ABTS method, indicating that the synthesized Tyr-Ala obtained by SPEPS showed a superior antioxidant capability compared with commercial glutathione.

Solid-Phase Total Synthesis of 1-β-Methylcarbapenem

A 1-b-methylcarbapenem analogue 6 was synthesized on polystyrene-diethylsilane resin (PS-DES) using 2-azetidinone bearing with 2-oxazolidone chiral auxiliary as starting material.

Solid-phase Synthesis of a Novel Kind of Hydroxylated Heterocyclic Ketene Aminals

An efficient solid-phase synthesis method for novel heterocyclic ketene aminals containing a hydroxyl group has been developed. The loading of the substrate on the resin through the hydroxyl group and the protection of the amine by the Schiff base were the key steps in the synthesis.

Design and Solid-Phase Synthesis of Multiple Muramyl Dipeptide (MMD)

As a non-specific modulator of macrophage, multiplied muramyl dipeptide (MMD) is solid-phase synthesized by application of standard Fmoc chemistry strategy. Tarn's multiple antigen system (MAS) is used as our four branched-linker on Lysine.

Polymer-support Selenium-induced Electrophilic Cyclization:Solid-phase Synthesis of Flavonoids

The Lewis acid mediated polystyrene supported selenium cyclization of chalcones and oxidative cleavage of selenium resins flavonoids in good yields and purities have been reported. induced intramolecular gave the corresponding

A Rapid Solid-phase Synthesis to Soluble Oligothiophene Molecular Wires

A novel method for the preparation of oligothiophene molecular wires is described via a bi-directional solid-phase synthesis. Using an alternating sequence of bromination and Stille coupling reactions, oligomers were obtained up to the heptamer in excellent yield and purity.

SOLID-PHASE SYNTHESIS OF 4,5-DISUBSTITUTED 1,2,3-TRIAZOLES

4-Aryl-5-ethoxycarbonyl-1-H-1,2,3-triazoles have been prepared by treatment of ethyl polystyrylsulfonylacetate with substituted benzaldehydes and then sodium azide.

Solid-phase Synthesis of Vinyl Sulfones Using Polystyrene-supported Selenomethyl Phenyl Sulfone

The solid-phase preparation of vinyl sulfones via a novel polystyrene-supported selenomethyl phenyl sulfone reagent has been reported.

Solid-phase Synthesis of Diethyl Trans-1-Aklenephosphonates Using Polymer-bound α-Diethoxyphosphoryl Methyl Selenide

The solid-phase preparation of diethyl trans-1 -alkenephosphonates via seleno-polymer reagent has been reported.

A SIMPLE,MANUAL SOLID-PHASE SYNTHESIS OF OLIGORIBONUCLEOTIDE

A simple,manual solid-phase synthesis of RNA fragments using 2'-(p-methoxyben- zyl)nucleosides and phosphoramidite chemistry is described.

Short Synthesis of C-terminal Modified Peptides by a Series-connection Procedure

Three peptide alcohols and four peptidyl N-akyl-amides were prepared by a series-connection procedure consisting of n-1 sequencial assembly on solid support followed by ammonolysis with glycinol, benzylamine or n-butylamine, and successive extractionelution through C-18 layer. All products were obtained from this procedure without further purification, in an overall yield of 75-86%.

An Efficient Synthesis of Cyclopeptides Bridged with Aliphatic-aryl Ether Bond

Based on the pseudo-dilution effect (PDE) on solid support, three cyclopeptides with an aliphatic-aryl ether bond as the bridge were synthesized via SN2 reaction between bromoacetylated at N-terminal and the phenol –OH group in C-terminal Tyr residue. All the products were obtained in good overall yields and characterized by related analytic data.

A New Route for the Synthesis of N-Substituted Diketopiperazine Derivatives

Eight N-substituted diketopiperazines （DKPs） were synthesized by solid-phase protocols. The introduction of iminodiacetic acid （Ida） and followed another a-amino acid residue as the precursor of DKP framework made the present synthesis to be very facile and efficient.