36 results about "Ugi reaction" patented technology

The invention provides a multi-component reaction preparing method for a functional nanometer porous polymer material. The multi-component reaction preparing method comprises the following steps: a, preparing an aldehyde reactant containing double bonds by a multi-component synthesis technology; b, utilizing 4-(allyloxy)benzaldehyde which is prepared in step a to realize Ugi four-component reaction so as to prepare a functional monomer; c, polymerizing reaction: using divinyl benzene as a crosslinking monomer, adding an initiator, and carrying out copolymerization reaction on the divinyl benzene and a proper quantity of Ugi reaction product by a solvothermal process so as to obtain the functional nanometer porous polymer material, wherein the mass ratio of the divinyl benzene to the functional monomer is 1.0-4.0, the mass ratio of the initiator to the divinyl benzene is 0.01-0.05, the mass ratio of a solvent to the divinyl benzene is 4.0-10.0, the polymerizing temperature is in a range between 60 DEG C and 200 DEG C, the pressure is controlled between 0.1MPa and 5.0MPa, and the reaction lasts for 12-48 hours.

The invention provides an amino acid based clustering peptide and a preparation method thereof and belongs to technical field of high polymer chemistry. The problem that an existing clustering peptide synthesis method is complicated in process, long in reaction cycle and restricted in practical application is solved. The structure of the amino acid based clustering peptide is shown as a formula I. The invention further provides the preparation method of the amino acid based clustering peptide. According to the method, amino acid or an amino acid derivative, aldehyde and fenvalerate are mixed in an organic solvent to obtain the amino acid based clustering peptide. The amino acid based clustering peptide is synthesized through Ugi reaction, the reaction conditions are mild, no catalyst is needed, the preparation process is simple, a reaction period is short, and experimental results show that the amino acid based clustering peptide with the concentration of 10 micro-g mL-1 to 100 micro-g mL-1 has a very good inhibiting effect on staphylococcus aureus, is superior to currently commercial epsilon-polylysine and has a good application prospect.

The invention discloses a self-repairing antibacterial hydrogel based on a borate bond. The self-repairing antibacterial hydrogel is prepared from a PEG derivative and polyvinyl alcohol; and the PEG derivative is prepared according to a method comprising the following step: performing a Ugi reaction on PEG-COOH, an aldehyde group-containing boric acid compound, a hydroxyl group-containing organicamine and isonitrile, wherein the PEG-COOH is carboxyl-terminated polyethylene glycol. According to the hydrogel provided by the invention, the polyethylene glycol derivative (PEG-Ugi) containing a boric acid group and a phenol structure is prepared by the Ugi reaction; when an aqueous solution of the PEG-Ugi and a PVA aqueous solution are mixed, the borate bond is formed by reacting the boronic acid group with a hydroxyl group in the PVA structure to rapidly form the hydrogel; the borate bond is a dynamic chemical bond, and the phenol structure has an antibacterial function, so that the obtained hydrogel has self-repairing ability and antibacterial properties, and is a novel antibacterial self-repairing hydrogel; and the method provided by the invention uses the raw materials which are safe, cheap and easy to obtain to prepare the hydrogel, the preparation method is simple, the gel forming conditions are mild, and the method has better application value.

The invention provides a functionalized nano-grade porous polymer material multicomponent reaction preparation method comprising the following steps: a, an aldehyde reactant comprising double bond is prepared through multicomponent synthesis; b, a Ugi four-component reaction is realized with 4-allyloxylbenzaldehyde prepared in the step a, such that a functional monomer is obtained; and c, divinyl benzene is adopted as a crosslinking monomer; an initiator is added; and divinyl benzene is subjected to a copolymerization reaction with a proper amount of the Ugi reaction product with a solvothermal method, such that the functionalized nano-grade porous polymer material is obtained. A mass ratio of divinyl benzene to the functional monomer is 1.0-4.0. A mass ratio of the initiator to divinyl benzene is 0.01-0.05. A mass ratio of the solvent to divinyl benzene is 4.0-10.0. The polymerization temperature is within a range of 60-200 DEG C. The pressure is controlled at 0.5-5.0MPa. The reaction time is 24-48h. After the reaction, residual solvent is removed through room-temperature volatilization or reduced-pressure distillation.

The invention relates to a method for constructing On-DNA alpha-amino amide compounds through aqueous-phase Ugi multi-component reaction, which is characterized in that amine, carboxylic acid, isocyanide and aldehyde are used as raw materials, and alpha-amino amide compounds with different structures are synthesized through Ugi reaction. The method can efficiently and quickly construct peptides, peptidomimetic compounds and various heterocyclic structure compounds, and is suitable for synthesizing a DNA coding compound library by using a porous plate.

The invention relates to a 5-(benzofuran-2-carbonyl)-6-carboxamide-5,6-dihydro-phenanthridine derivative and synthesis and application thereof. Firstly, benzofuran-2-formamide is obtained through Ugi reaction of arylamine, 2-bromoacetic acid, 2-bromobenzaldehyde and substituted isonitrile and subsequent microwave-assisted Rap-Stoermer reaction; and then, a reactant (benzofuran-2-formamide), a metal palladium catalyst, a ligand, an additive and alkali are added to an anhydrous organic solvent, and the mixture is heated, reacted and subjected to aftertreatment after reaction is completed to obtain the high-purity 5-(benzofuran-2-carbonyl)-6-carboxamide-5,6-dihydro-phenanthridine derivative. In the preparation method provided by the invention, the raw materials are simple and easy to obtain, the operation is easy and convenient, aftertreatment is easy, diversified substituents are easy to obtain, and the generated compound contains two important heterocyclic structures of benzofuran-2-formamide and dihydro-phenanthridine simultaneously, and can well meet the demand for screening of pharmaceutical activity, thereby having good application and market values in the preparation of anti-hepatitis B virus medicaments.

The invention relates to an quinoxaline-azetidinones compound preparation and an application of the quinoxaline-azetidinones compound in tumor resistance. According to the invention, a Ugi reaction is taken as a base, under microwave assistance, azetidinone is obtained through ring closure under diisopropylamine condition, then quinoxaline ring is obtained in a trifluoroacetic acid / dichloroethanes solution with concentration of 10%, and the quinoxaline-azetidinones compound has latent antitumor activity.

The invention relates to a dearomatization-based novel 1,4 addition type Ugi reaction. The reaction includes steps: taking a 15ml pressure-resistant reaction tube, adding 2mL of trifluoroethanol, sequentially adding imine, acid and t-butylisonitrile into the pressure-resistant reaction tube, tightly plugging, stirring for 10min, transferring the reaction tube into an oil bath at 60 DEG C, and monitoring an extent of reaction by a thin layer chromatography silicon rubber plate until reaction is finished. Aniline is oxidized into imine by iodobenzene diacetate, then imine is subjected to reaction with carboxylic acid and t-butylisonitrile, and trifluoroethanol serves as a solvent.

The invention relates to a method for synthesizing 2,5-dicarbonyl piperazine compounds. In the reaction, the solvent is methyl alcohol, the reaction temperature is 45 DEG C, reaction time is 10-20 hours, the R1 is 4-methyl phenyl, n-propyl or benzyl, the R2 is methoxy acyl or ethoxy acyl, the aldehyde is heteroaromatic aldehyde with heteroatom at alpha site. The aldehyde used in the Ugi reaction is heteroaromatic aldehyde with heteroatom at alpha site, so that the heteroatom at the aromatic ring and the amide in the Ugi product can form intramolecular hydrogen bond, Micheal reaction is promoted to be carried out smoothly, the purpose of mild reaction condition is realized, all the reactions are finished once and are convenient and rapid.

The invention relates to a preparation method and application of carbazole derivatives. On the basis of a four-component Ugi reaction, the carbazole derivatives are synthesized through cyclization ofsynthesized intermediates by a microwave assisted reaction in a DMF (dimethyl formamide) solvent on the basis of no purification. The carbazole derivatives have antitumor activity.

The invention relates to the field of biopolymer materials and particularly relates to a modified polymannuronic acid derivative, a drug-carrying aqueous emulsion and a preparation method thereof. Low-molecular-weight polymannuronic acid as a raw material undergoes an Ugi reaction to produce an amphiphilic polymannuronic acid derivative. The surface activity test result shows that the derivative has a low critical aggregation concentration and good surface activity, can be used as a water emulsion stability aid and has a good regulation effect on the stability and drug release of the emulsion.

The invention relates to a preparation method and application of carbazole derivatives. On the basis of a four-component Ugi reaction, the carbazole derivatives are synthesized through cyclization ofsynthesized intermediates by a microwave assisted reaction in a DMF (dimethyl formamide) solvent on the basis of no purification. The carbazole derivatives have antitumor activity.

The invention relates to an quinoxaline-azetidinones compound preparation and an application of the quinoxaline-azetidinones compound in tumor resistance. According to the invention, a Ugi reaction is taken as a base, under microwave assistance, azetidinone is obtained through ring closure under diisopropylamine condition, then quinoxaline ring is obtained in a trifluoroacetic acid / dichloroethanes solution with concentration of 10%, and the quinoxaline-azetidinones compound has latent antitumor activity.

The invention relates to flame retardants containing melamine structure as well as a preparation method and application thereof. The chemical structural formula of the flame retardants is shown in thedescription, wherein substituent groups R1, R2 and R3 are any one of hydrogen, tertiary butyl, normal-butyl, cyclohexyl alkyl or chlorine, bromine, methyl, methoxy, nitryl, amino, hydroxy-substitutedaryl or ceteroary. A synthesis method comprises the following steps: carrying out Ugi reaction on carboxylic acid compounds, the melamine, aldehyde compounds and isonitrile compounds in a mixed solvent of methanol and isopropanol at the temperature of 50 DEG C under the concerted catalysis of an MCM-41-loaded copper complex, MIL-101 and p-toluenesulfonic acid; carrying out filtering, extracting and column chromatography on a product to obtain the flame retardants containing the melamine. The invention discloses a novel preparation method with the advantages of simple reaction, few byproductsand better selectivity, which is used for selectively synthesizing the melamine flame retardants. The flame retardants disclosed by the invention have the advantages of good thermal stability, high flame retardancy rate, high purity reaching to 97.2 percent, easily-obtained raw materials, advanced technology and easiness for industrial production.

The invention discloses a preparation method of N-(indole-N-formyl)-α-aminoamide derivatives, which comprises the following steps: N-indole carboxylic acid compounds, aldehyde compounds, primary amine compounds and The four-component reaction of the isonitrile compound in the solvent; or the three-component reaction of the N-indole carboxylic acid compound, the cyclic imine compound and the isonitrile compound in the solvent. After the reaction is completed, the post-treatment obtains the N-(indole-N-formyl)-α-aminoamide derivative; the preparation method uses the indole compound as a potential component of the classic Ugi reaction, in mild The rapid connection of indole skeleton and α-aminoamide is realized under the conditions, the reaction is efficient, concise and fast, and the yield is high, which has far-reaching significance for organic synthesis and medicinal chemistry.

The invention relates to a preparation method of a benzodiazepine compound, which comprises the following steps: reacting amino functionalized ionic liquid, phenylpropyl aldehyde, Boc-anthranilic acid and cyclohexyl isonitrile to obtain an ionic-liquid-loaded Ugi product; reacting the ionic-liquid-loaded Ugi product under the catalytic action of hydrogen chloride gas to obtain a benzodiazepine compound of which the side chain is modified by Ugi reaction; and carrying out rotary evaporation on the reaction liquid, and washing out residues with anhydrous aether to obtain the required benzodiazepine compound. Compared with the existing preparation method, the preparation method provided by the invention shortens the reaction procedures and enhances the reaction efficiency; and the synthesis method is simple and efficient, and has wide application prospects.

The invention provides an amino acid based clustering peptide and a preparation method thereof and belongs to technical field of high polymer chemistry. The problem that an existing clustering peptide synthesis method is complicated in process, long in reaction cycle and restricted in practical application is solved. The structure of the amino acid based clustering peptide is shown as a formula I. The invention further provides the preparation method of the amino acid based clustering peptide. According to the method, amino acid or an amino acid derivative, aldehyde and fenvalerate are mixed in an organic solvent to obtain the amino acid based clustering peptide. The amino acid based clustering peptide is synthesized through Ugi reaction, the reaction conditions are mild, no catalyst is needed, the preparation process is simple, a reaction period is short, and experimental results show that the amino acid based clustering peptide with the concentration of 10 micro-g mL-1 to 100 micro-g mL-1 has a very good inhibiting effect on staphylococcus aureus, is superior to currently commercial epsilon-polylysine and has a good application prospect.

The invention relates to a preparation method and application of a condensed benzimidazole azetidinone derivative. The method comprises the steps of performing ring closure into azetidinone under an alkaline condition based on a Ugi reaction, and then obtaining a benzimidazole ring under an acidic condition. The condensed benzimidazole azetidinone derivative has potential anti-tumor activity.

The invention relates to the field of biopolymer materials and particularly relates to a modified polymannuronic acid derivative, a drug-carrying aqueous emulsion and a preparation method thereof. Low-molecular-weight polymannuronic acid as a raw material undergoes an Ugi reaction to produce an amphiphilic polymannuronic acid derivative. The surface activity test result shows that the derivative has a low critical aggregation concentration and good surface activity, can be used as a water emulsion stability aid and has a good regulation effect on the stability and drug release of the emulsion.

The invention relates to a preparation method and application of a 4-hydroxyquinolinone derivative. Based on Ugi reaction and under the alkaline condition, a quinolinone compound is formed through ring closing. The 4-hydroxyquinolinone derivative has latent anti-tumor activity.

The invention relates to a preparation method and application of uracil derivatives. On the basis of a Ugi reaction, carboxylic acid, methyl-2-aminobenzoate, ethyl glyoxalate and isocyanide are used as raw materials, and the uracil derivatives are synthesized in a one-pot mode under the alkaline condition with the assistance of microwaves. The synthesizing method has the advantages of being simple in operation, short in synthesizing route, low in cost and the like, and is suitable for quick synthesis of the uracil derivatives.