21 results about "Nitrone" patented technology

The invention discloses an application of nitrone compounds in preparation of related products for improving athletic ability. The nitrone compound disclosed by the invention has a structure shown in a general formula (I), and experimental results show that the nitrone compound disclosed by the invention can be used for increasing the exercise capability of nematodes of different age groups, including the body swing frequency and the pharyngeal pumping rate.

The application discloses application of a nitro compound in preparation of products prolonging life, and the nitro compound has the structure shown in the following general formula (I). The application takes Caenorhabditis elegans as an object, and studies influence of TBN on life and health indexes of the Caenorhabditis elegans. Experimental results show that the TBN prolongs the life of the Caenorhabditis elegans, significantly improves pharyngeal pumping rate and movement ability of the Caenorhabditis elegans, and significantly reduces lipofuscin accumulation degree of the Caenorhabditis elegans.

The invention relates to fluorine-containing isoxazolidine-5-ketone as well as a synthesis method and anti-tumor application thereof. According to the synthesis method, gem-difluorocycloacrylimide and nitrone are taken as substrates, Ni (ClO4) 2.6 H2O is taken as a catalyst, (+ / -)-2, 2 '-(propane-2, 2-diyl) bis (4-phenyl-4, 5-dihydrooxazole) is taken as a ligand (L) in an organic solvent, cycloaddition isomerization reaction is carried out at about 30 DEG C, and the fluorine-containing isoxazolidine-5-ketone compound is obtained. And the fluorine-containing isoxazolidine-5-ketone is obtained through preparation. The method is mild in reaction condition, capable of being well compatible with various functional groups and high in yield, and the product further has certain biological activity and can inhibit proliferation of cancer cells. The invention discloses the realization of the cycloisomerization reaction of the gem-difluorocyclopropene and the nitrone for the first time, provides a new idea for the synthesis of the fluorine-containing isoxazolidine-5-ketone and the derivative thereof, and has a good application prospect in the fields of medicines and synthesis.

The application discloses a catalytic synthesis method of chiral polysubstituted hydrogenated quinoline compounds, and belongs to the field of organic synthesis. The application comprises the following steps: at 0-40 DEG C, alcohol or halogenated alkane is used as a solvent, a copper metal catalyst and a chiral ligand are added, and reaction is carried out under nitrogen protection for 0.5-2 hours; the temperature is lowered to-60-0 DEG C; then, o-aminophenyl nitrone, propargyl alcohol ester and alkali are sequentially added; and reaction is carried out for 6-48 hours, so as to obtain a chiral polysubstituted hydrogenated quinoline compound shown in formula 1 or 2. The application realizes, for the first time, synthesis of chiral polysubstituted hydrogenated quinoline compounds by using o-aminophenyl nitrone and propargyl alcohol ester as reactants, and by using a cheap copper metal catalyst and a chiral ligand, the method is simple in operation, low in cost, and has excellent enantioselectivity and diastereoselectivity.

This invention discloses an isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compound, its preparation method, and its applications, belonging to the field of organic compound synthesis technology. Using N-indole-linked o-alkynyl nitrone compounds as raw materials, this invention employs a two-step, one-pot method to provide a novel synthesis of isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compounds that are difficult to prepare using conventional methods. This method is based on a rhodium-catalyzed internal redox / dearomatization [3+2] cycloaddition reaction and a cerium ammonium nitrate-promoted oxidative debenzylation / spirocyclic tandem reaction strategy. The method of this invention has advantages such as simple operation, low catalyst loading, broad substrate range, single stereoselectivity, and high yield. The isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compound prepared by this invention has a certain inhibitory effect on plant pathogens and can be potentially applied to the control of tomato gray mold, wheat scab, and rice sheath blight.

The invention belongs to the field of chemical synthesis, particularly relates to an N, N-disubstituted hydroxylamine compound and a synthesis method and application thereof, and provides an efficient method for reducing 1, 3-dipolar nitrone into the N, N-disubstituted hydroxylamine compound, on the basis of nitrone synthesis, nitrone is reduced by taking trichlorosilane as a reducing agent, and the N, N-disubstituted hydroxylamine compound is obtained. The hydroxylamine compound is suitable for a plurality of different substituted benzene rings or heterocyclic compounds. The synthesis method has the characteristics of high efficiency, greenness, mild conditions, wide substrate application range and the like, and provides a new thought for synthesis of the hydroxylamine compound.

The invention discloses application of a nitrone compound in preparation of a product for prolonging the service life, the nitrone compound has a structure as shown in the following general formula (I), caenorhabditis elegans is taken as an object, and the influence of TBN on the service life of the caenorhabditis elegans is researched; experimental results show that the TBN can significantly prolong the service life of caenorhabditis elegans.

The invention relates to the technical field of organic synthetic chemistry, in particular to a synthetic method of heterocyclic aromatic nitrone, which comprises the following steps: S1, mixing heterocyclic aromatic compound and phenyl nitrone in a molar ratio of 1: (1-1.5) with a catalyst, adding an organic solvent, and dissolving to obtain a mixture solution; and S2, reacting the mixture solution in the step S1 at 20-30 DEG C for 1-6 hours, carrying out reduced pressure distillation to remove the organic solvent, and carrying out column chromatography purification to obtain the aromatic heterocyclic nitrone. The synthesis method of the heterocyclic aromatic nitrone, which adopts the steps, has the advantages of mild reaction conditions, high heterocyclic aromatic nitrone yield and short reaction time, and can be used for gram-level reaction.

The invention provides a synthesis method of a gamma-boryl alkylamine compound, and belongs to the field of organic synthesis and fine chemicals. According to the method, olefin is used as a reaction raw material, bis (pinacol) diboron (B2pin2) is used as a boron source, carbene copper is used as a catalyst, nitrone is used as an electrophilic reagent, beta-boryl alkyl copper generated by olefin is captured, an obtained intermediate is not separated, sodium triacetoxyborohydride is used for reduction, and the gamma-boryl alkylamine compound is successfully prepared through a one-pot two-step method. According to the method, commercially available carbene copper is used as a catalyst, olefin and nitrone which are low in price and easy to obtain are used as raw materials, the reaction condition is mild, the substrate application range is wide, and excellent regioselectivity is achieved. The method disclosed by the invention has important significance in the fields of medicines, materials, fine chemical engineering and the like.

The application discloses a preparation method of adamantane nitroketone derivatives and application of the adamantane nitroketone derivatives in ischemic stroke drugs. The adamantane nitroketone derivatives are combined by 2,3,5,6-tetramethylpyrazine and adamantane compounds through nitroketone. The compound not only has strong free radical scavenging capacity, but also integrates the nerve protection function of the adamantane compound.

The invention discloses a copper monatomic catalyst with stable N-heterocyclic carbene as well as a preparation method and application of the copper monatomic catalyst with stable N-heterocyclic carbene. According to the method, construction of a porous organic polymer carrier and anchoring of metal monatomic active sites are innovatively combined, and the copper monatomic catalyst with stable N-heterocyclic carbene is prepared through a one-pot mechanical grinding strategy. A triazine compound, a nitrogen-containing heterocyclic compound, a copper salt and alkali directly react under the assistance of no solvent or a trace amount of solvent, and the catalyst POP-n-NHC-CuX (n = I-IV, X = Cl, Br or I) is obtained through in-situ synchronous synthesis. In the obtained catalyst, copper atoms are stably anchored on a polymer skeleton in a coordination bond form through an NHC ligand to form atomic-scale dispersed active sites. The catalyst can efficiently catalyze the conversion reaction of CO2 and propargyl alcohol and derivatives thereof under mild conditions, is suitable for synthesizing various high value-added chemicals including alpha-alkylene cyclic carbonate, oxazolidinone and beta-oxypropyl carbamate, and shows excellent catalytic cycle stability and substrate universality.

The invention provides application of a nitrone compound as shown in a formula I, a nitrone compound as shown in a formula II and / or a nitrone compound as shown in a formula III as a precursor for generating an isoxazolidine mosquito repelling component and / or an isoxazolidine cooling component. In the formula # imgabs0, R is Me, Et, n-Pr, i-Pr, Cy, t-Bu or Bn. The nitrone compound is used as a precursor of the isoxazolidine mosquito-repelling component and / or the isoxazolidine cooling component for the first time, the isoxazolidine mosquito-repelling component and / or the isoxazolidine cooling component are / is generated by heating to reach the initial ring closing temperature or above, and the repelling rate of the generated isoxazolidine mosquito-repelling component after 24 hours is 100%; the mosquito repelling effect is good, A-level mosquito repelling is achieved, and the generated isoxazolidine mosquito repelling component also has aroma and cooling effects. As a precursor of an isoxazolidine mosquito-repelling component, the nitrone compound can be stored for a long time when mosquito repelling is not needed; when mosquito repelling is needed, release of mosquito repelling components can be controlled by adjusting the heating temperature, and the purposes of slow release and long-acting mosquito repelling are achieved; as a precursor of an isoxazolidine cooling component, the nitrone compound can be stored for a long time when cooling is not needed; when cooling is needed, release of cooling components can be controlled by adjusting the heating temperature, and the purposes of slow release and long-acting cooling are achieved.

The invention provides chiral annular nitrone and a preparation method thereof, and belongs to the technical field of organic synthetic chemistry. The method comprises the following steps: by taking alkenyl oxime and aryl halide as raw materials, adding a palladium catalyst, a chiral ligand and alkali, then adding an organic solvent under the protection of inert gas, and reacting at 50-100 DEG C for 12-24 hours. And after the reaction is finished, carrying out silica gel column chromatography separation to obtain the chiral annular nitrone. According to the invention, the palladium catalyst is combined with the chiral ligand to realize intermolecular cyclization of alkenyl oxime and aryl halide to generate chiral annular nitrone. The reaction enantioselectivity is good, generation of a Heck product and an oxygen heterocyclic ring product oxime ether is avoided, the highest yield can reach 90%, the highest ee value can reach 98%, the conditions are mild, the yield is high, and the method has a very good application prospect.

There is provided a polymer system for producing a hydrogel. The system has two components. A first component comprising a first synthetic polymer and a gel former and a second component comprising a second synthetic polymer. The first synthetic polymer is functionalized with a first click chemistry group and the second synthetic polymer is functionalized with a second click chemistry group that reacts with the first click chemistry group to form a covalent link by click chemistry. One of the first click chemistry group or the second click chemistry group comprises a cycloalkene, a heterocycloalkene, a cycloalkyne or a heterocycloalkyne and the other comprises an azide, a tetrazine, a triazine, a pyridazine, an oxime, a nitrone or nitrile-oxide. The gel former has a gelation mechanism that is independent from the click chemistry.

The invention discloses a trifluoromethyl-containing isoxazolidine compound as well as a synthesis method and pharmaceutical application thereof, and belongs to the technical field of pharmaceutical synthesis. Beta-trifluoromethyl-alpha, beta-unsaturated ketone compounds 1 and N-benzyl nitrone 2 are used as raw materials, and in the presence of chiral binaphthol ligands or tetrabenzocyclooctadiene ligands, triphenyl borate and molecular sieves, asymmetric [3 + 2] cycloaddition reaction is performed to obtain the optically active trifluoromethyl-containing isoxazolidine compounds 3. The synthesis route has the advantages of easily available raw materials, mild reaction conditions, high catalytic efficiency and the like, and the obtained product shows remarkable physiological activity on cervical cancer C33A, lung cancer A549, breast cancer MCF-7, colon cancer HCT116 cells and the like, and provides an effective way for development of novel anticancer lead compounds.

This invention discloses a method for preparing hydroxylamine compounds by reducing nitroketone compounds without a metal catalyst. This method uses benzylsilane as a hydrogen source and toluene as a solvent, requiring no additional metal catalyst. The reduction product is obtained by stirring the reaction at 70–80°C under inert gas protection and a closed system. This invention employs a metal catalyst-free system for the reduction of nitroketone compounds, offering advantages such as low cost, mild reaction conditions, and high selectivity. It avoids the use of special equipment such as hydrogen and autoclaves, as well as excessive sodium borohydride reducing agents.

The application discloses a preparation method of 2-aryl-2,3,4,5-tetrahydro-1,4-epoxybenzoazepine compounds, which couples a nitro compound with an allyl precursor compound through Rh(III) catalysis, realizes C-H allylation, and then realizes 1,3-dipolar cycloaddition in a molecule to realize synthesis of a target compound in one step. The method has the advantages of simple synthesis route, wide substrate range, efficient preparation process, high yield and good application prospect.

Disclosed herein are nitrones that are capable of forming 4-isoxazoline compounds by strain-promoted alkyne-nitrone cycloaddition (SPANC), which have improved stability. The 4-isoxazoline compounds do not disintegrate by rearrangement into two molecules. The nitrone compounds disclosed herein are suitable for preparing bioconjugates by SPANC reaction. Also disclosed herein are the thus obtained bioconjugates, as well as the application thereof in targeting cells and treating cancer.

Provided is use of a nitrone compound in the preparation of a product for preventing or treating side effects caused by anti-obesity drugs. Animal experiments have found that combined use of the nitrone compound with glucagon-like peptide-1 drugs does not affect the ability of the glucagon-like peptide-1 drugs to reduce the fat mass of mice, and can also resist / weaken the side effects caused by the glucagon-like peptide-1 drugs. Moreover, after the use of the glucagon-like peptide-1 drugs is stopped, the continuous administration of the nitrone compound can also delay the speed of body weight rebound after drug withdrawal, especially the speed of fat mass rebound. The nitrone compound can effectively prevent or treat the side effects caused by the glucagon-like peptide-1 drugs, and thus has important clinical significance.

The invention relates to a method for preparing an aryl thiopyrano [3, 2-e] [1, 2] oxazine compound. According to the method, an N-methyl aryl nitrone compound and an aryl thioether cyclopropane compound react through photocatalysis. Comprising the following steps: step 1, loading magnetons into a dried 10mL Schlenk tube, adding a photocatalyst C (solid) and a raw material A (solid), extracting and replacing nitrogen for three times, rapidly adding ultra-dry acetonitrile under nitrogen flow, rapidly adding the raw material A (liquid) by using a microsyringe, and tightening a cock to obtain a mixed solution; wherein the raw material A is N-methyl aryl nitrone, the raw material B is aryl thioether cyclopropane, and the photocatalyst C is Acr-Mes-tBu < + > (BF4 <->). And 2, stirring the mixed solution obtained in the step 1 at room temperature under the irradiation of 456nm blue light until the N-methyl aryl nitrone compound is completely reacted, and after the reaction is finished, carrying out silica gel column chromatography separation on the reaction solution to obtain the aryl thiopyrano [3, 2-e] [1, 2] oxazine compound. Compared with other methods for synthesizing the oxazine compounds, the preparation method disclosed by the invention has the advantages that the conditions are mild, the dosage of the used nonmetal catalyst is small, the cost is low, the substrate application range is wide, and the obtained aryl thiopyrano [3, 2-e] [1, 2] oxazine compounds have wide application prospects in research and development of medicines, agricultural chemicals and advanced materials.

The invention belongs to the technical field of medicines, and discloses a magnolol / honokiol nitrone derivative as well as a preparation method, a pharmaceutical composition and application thereof. Specifically, the invention discloses magnolol / honokiol nitrone derivatives as shown in a general formula I and a general formula II. The derivatives are prepared in an artificial synthesis mode, pharmaceutical compositions containing the derivatives and application of the derivatives in the anti-inflammatory aspect.