61 results about "Combinatorial chemistry" patented technology

Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.

The invention discloses a trivalent copper catalyst and a preparation method thereof and application to hydrochlorination of acetylene. The preparation method of the trivalent copper catalyst comprises the steps that a nitrogen-containing heterocyclic compound and copper salt are added into a trichloromethane solution to mix to obtain a mixed solution A containing a bivalent copper compound; ionicliquid is added into the obtained mixed solution A, and under the action of an oxidant, a mixed solution B containing a trivalent copper compound is obtained; and a porous solid carrier is immersed in the obtained mixed solution B containing the trivalent copper compound for 0.5-5 h, then the treated solid is taken out, and heated and dried under the condition of blue light irradiation, and the trivalent copper catalyst is obtained. The trivalent copper catalyst is used for the reaction of acetylene hydrochlorination to prepare vinyl chloride. The trivalent copper catalyst is prepared by simple operation steps, the stability and activity of the catalyst are improved, the production cost is lowered, and good application prospect is achieved.

The invention relates to a tilmicosin soluble powder. The tilmicosin soluble powder is characterized by comprising the following ingredients in percentage by mass: 5-25% of tilmicosin, 3-15% of a cosolvent, 1-3% of a solubilizer, 3-8% of PEG and filler. The invention further provides a preparation method of the tilmicosin soluble powder. According to the tilmicosin soluble powder and the preparation method thereof disclosed by the invention, the preparation process is simple, only simple mixing is needed, the raw materials are all commercially available, low in price and easily available, and the obtained compound preparation is stable in performance; because of addition of the cosolvent and the solubilizer, the tilmicosin soluble powder is good in dissolving property, quite suitable for applications in clinic aspects, capable of meeting the relevant provisions of pharmacopoeia, suitable for industrialized large-scale production, and quite wide in application prospect. The tilmicosin soluble powder has a high practical value.

The invention discloses a synthetic method for a chiral quaternary carbon oxazolidinone compound. The synthetic method comprises the following steps: taking o-hydroxy chalcone and azlactone as reactants and synthesizing in a solvent under the catalysis of chiral multifunctional chiral quinine thiourea to obtain a product. The synthetic method disclosed by the invention has the advantages that raw materials are easy to obtain, the reaction conditions are mild, the post-treatment is simple and convenient, the applicable substrate scope is wide, the yield is high, and the enantioselectivity is high; the product obtained by the synthesis method can be used for synthesizing an intermediate of a drug and a pesticide.

The present invention relates to a method for preparing t-butyl 2-((4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxan-4-yl)acetate having optical activity, which is a core intermediate in the preparation of a variety of HMG-CoA reductase inhibitors. According to the preparation method of the present invention, it is possible to easily mass-produce t-butyl 2-((4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxan-4-yl)acetate in the form of a solid of high and uniform purity by using a polymer-supported TEMPO.

The invention belongs to the technical field of regenerated fibers, and particularly relates to an antibacterial and antiviral regenerated cellulose fiber and a preparation method thereof. The antibacterial and antiviral regenerated cellulose fiber comprises a viscose fiber, a single-layer capsule wall composite microcapsule and a double-layer capsule wall composite microcapsule; capsule cores inthe single-layer capsule wall composite microcapsule and the double-layer capsule wall composite microcapsule independently comprise plant antibacterial and antiviral extracts and vitamins; componentsof a capsule wall of the single-layer capsule wall composite microcapsule comprises beta-cyclodextrin, a capsule wall of the double-layer capsule wall composite microcapsule comprises an inner-layercapsule wall body and an outer-layer capsule wall body, components of the inner-layer capsule wall body comprise beta-cyclodextrin, and components of the outer-layer capsule wall body comprise porousstarch; and the capsule wall of the single-layer capsule wall composite microcapsule is grafted and cross-linked with a bonding fiber, and the capsule wall of the double-layer capsule wall composite microcapsule is grafted and cross-linked with the viscose fiber. The antibacterial and antiviral regenerated cellulose fiber can avoid the loss of effective components; and meanwhile, the persistence of the effective components in playing a role can be improved.

The invention relates to a preparation method of D-p-hydroxyphenylglycine methyl ester. The preparation method comprises the following steps: (1) esterifying: carrying out an esterification reaction on D-p-hydroxyphenylglycine and methanol to obtain D-p-hydroxyphenylglycine methyl ester sulfate, and distilling off methanol and water under reduced pressure, wherein the D-p-hydroxyphenylglycine is added one time, and the methanol is added in batches; and (2) crystallizing the D-p-hydroxyphenylglycine methyl ester. The preparation method can very easily control the reaction endpoint, so that theyield and the quality index of the finished product can be guaranteed to the maximum extent; the preparation method provided by the invention avoids the problems of safety and operation caused by hydrogen chloride gas or thionyl chloride; and in the step of D-p-hydroxyphenylglycine methyl ester crystallization, an alkali metal hydroxide is used for adjusting the pH value of the system without using ammonia water, so that the problem that ammonia ions are difficult to treat is avoided.

The invention relates to the technical field of separation of a natural free radical scavenger in Saxifraga atrata Engl, in particular to a separation preparation process and application of the natural free radical scavenger in Saxifraga atrata Engl. The preparation process comprises the following seven steps: extraction, online free radical scavenger component screening, microporous resin columncoarse separation, online free radical scavenger screening, reversed-phase preparative column preparation, reversed-phase preparative liquid chromatography purification of components Fr4-1 and Fr4-2,and hydrophilic preparative liquid chromatography purification of components Fr4-3 and Fr4-4. The method is low in cost, and the product purity is greater than 95%; the technical means adopted by theinvention can be used for large-scale production: the raw material requirement is not high, the cost is low, and batch preparation is easy; methanol room-temperature cold leaching extraction is adopted, and operation is easy; a microporous resin column is adopted for coarse separation, and the microporous resin separation material can be arranged in a medium-pressure column chromatography system and is easy for large-scale production; a reversed-phase preparative liquid chromatography or a hydrophilic preparative liquid chromatography used in separation and purification is a rapid isocratic method.

The invention discloses a Ni3P/SiO2 catalyst as well as a preparation method and application thereof. The Ni3P/SiO2 catalyst is composed of a SiO2 carrier and Ni3P loaded on the SiO2 carrier, the mass percent of Ni3P in the catalyst is 10-45%, the balance is the SiO2 carrier, the particle size of Ni3P in the catalyst is 6-15 nanometers, and the specific surface area of the catalyst is 50-250 m<2>/g. Experiments show that the Ni3P/SiO2 catalyst provided by the invention is high in activity, high in selectivity and good in stability, especially has the advantages that the selectivity of methyl glycolate can still reach 85% or above under deep conversion of dimethyl oxalate (greater than 99.9%), a high-selectivity temperature window is wide and the like, and can be used as a catalyst for a reaction of preparing methyl glycolate through hydrogenation of dimethyl oxalate; and in addition, the preparation method disclosed by the invention is simple, mild in condition and easy to realize large-scale production.

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:

wherein one of Q and T represents a group represented by the general formula:

while the other represents a lower alkyl group or a halo(lower alkyl) group; R¹ represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R² represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

The invention discloses a small micelle nano-drug and a preparation method and application thereof. A micromolecule drug and an amphiphilic polymer/targeted amphiphilic polymer are added into polycthylene glycol oilgomers to obtain a mixed solution, then the mixed solution is added into a buffer solution to obtain the small micelle nano-drug; and the molecular weight of the polycthylene glycol oilgomers is 200-600. The invention designs and prepares an efficient paclitaxel PTX-loaded micelle MPTX, a disulfide cross-linked micelle MPTX and three TNBC active targeting micelle nano-drug, the drug loading capacity is up to 23.1 wt.%, the particle size is less than 40 nm, and the micelle nano-drug has good stability and drug release performance of reduction response.

The invention provides a chlorphenamine maleate oxidation impurity, which has the structure defined in the specification. The invention also provides a preparation process of the chlorphenamine maleate oxidation impurity. According to the invention, the experiment results prove that the chlorphenamine maleate oxidation impurity generally exists in a chlorphenamine maleate finished product, and thestructure of the chlorphenamine maleate oxidation impurity is close to the structure of chlorphenamine maleate, so that the separation difficulty is relatively high; and the chlorphenamine maleate oxidation impurity is prepared by a simple process, can be used as a reference substance for quality control of chlorphenamine maleate, and has good application prospect.

The invention discloses a quinolizine aza-bis-aromatic ring axial chiral compound and a synthesis method of the quinolizine aza-bis-aromatic ring axial chiral compound. The method comprises the following steps: firstly obtaining an intermediate from raw materials substituted 1-naphthyne and methyl chloroformate under the action of lithium diisopropylamide, then generating a precursor from the intermediate and 2-methylpyridine under the action of lithium diisopropylamide, and finally reacting the precursor under the action of CuCl and a chiral phosphamide ligand to obtain the quinolizine aza-bis aromatic ring axial chiral compound. The method disclosed by the invention is mild in reaction condition and extremely high in yield and enantioselectivity, the quinolizine aza-bis-aromatic ring axial chiral compound taking quinolizine as a matrix is synthesized for the first time, and the range of the aza-axial chiral compound is greatly expanded.

The invention discloses a PEG modified polymyxin or medicinal salt shown in the formula I and a preparation method and application of the PEG modified polymyxin or medicinal salt. The PEG modified polymyxin is a stable compound formed by connecting PEG molecules to polymyxin through covalent bonds. The molecular weight of the PEG modified polymyxin is multiplied, the half-life period is prolonged, and the aims of enhancing the treatment effect and reducing toxicity are achieved. Please see the molecular formula I in the description.

The invention discloses a method for preparing obeticholic acid intermediate and obeticholic acid thereby, wherein the obeticholic acid intermediate is prepared with 3A-hydroxy-6-vinyl-7-oxo-cholanicacid as a raw material through carbonyl reduction and hydroxyl protection. The obeticholic acid intermediate has two benzene ring structures and has strong ultraviolet absorption, so that quality researching can be carried out by means of an ultraviolet detector, thus guaranteeing mass controllability of the raw material in the last one step. At room temperature, the intermediate is a solid, and can be purified through regular purification methods such as recrystallization. Then through Pt/C catalyst for reduction, the obeticholic acid is obtained. In the aspect of reaction process, firstly, the reduction of the olefinic bond is completed in the Pt/C catalytic reduction, so that the reaction is convenient to trace. The method is high in reaction yield and is complete in conversion, so thatpurification difficult of the finish product is reduced.

The invention provides a low-cost new method for synthesizing a N-vinyl azole compound from a n azole compound and a propargyl tertiary sulfur salt compound under the promotion of a common inorganic base. According to the invention, the synthesized N-vinyl azole compound is an important structural unit of medicines, semiconductors and photosensitive materials, so that the synthesis method providedby the invention has very important commercial value.

The invention discloses an ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof, and belongs to the field of chemical biology. According to the presentinvention, the active molecular probe is designed and synthesized through structure modification based on the parent compound Rg3, can achieve the recognition and labeling of the drug action target inliving cells, has antitumor activity similar to Rg3, and provides the advantageous tool in the research on the antitumor action target and the action mechanisms of Rg3.

This invention relates to methods, which provide access to F-18 labeled stilbene derivatives.

The invention relates to a hypoglycemic peptide and an application thereof. A long-acting derivative is obtained by structural modification of insulin. The invention also discloses a novel compound used for modification and a preparation method thereof, and the hypoglycemic peptide of the invention is synthesized by solid phase synthesis by an orthogonal protection strategy, the synthesis method is simple, and the synthesis speed is fast. Moreover, the hypoglycemic peptide has the significant hypoglycemic effect and a long acting time.

The invention discloses a preparation method of a tertiary amide compound, and belongs to the field of organic synthesis. The tertiary amide compound represented by formula (I) is prepared by directlycoupling an aryl formamide compound represented by formula (II) with a p-toluenesulfonylhydrazone compound represented by formula (III) under the action of a specific copper catalyst and an alkali reagent without ligand participation and a high-temperature reaction system. The method is green, simple and convenient, and the yield of the tertiary amide compound can reach about 82%.

The present invention provides a method which enables the simple, economical and high-yield production which is a key intermediate of antidiabetic drug Januvia.

The present invention relates to a toluene diisocyanate purification method enabling acquisition of a product having a small amount of dimers in a final product by means of using a reactive dividing wall column during toluene diisocyanate preparation. More particularly, according to the present invention, in order to obtain a product having a small amount of dimers in accordance with a reversible reaction of a monomer and a dimer, a purification procedure is designed by means of applying the temperature, pressure, time of stay and the like of a reactive dividing wall column as appropriate particular conditions, a reboiler having short time of stay and high heat transfer rate is used, and thus a dimerization reaction is inhibited and the purity and yield of the product are enhanced. Therefore, high-purity toluene diisocyanate can be purified and obtained.

The invention relates to a catalyst and a method for preparing p-methyl benzaldehyde from synthesis gas and toluene. The catalyst and the method for preparing p-methyl benzaldehyde from synthesis gasand toluene are characterized in that: a copper-zirconium bimetallic catalyst is used as a main catalyst, and an H-ZMS-5 molecular sieve or an H-ZMS-11 molecular sieve is used as a carrier. The raw material cost is low, one-step preparation method is adopted, the process route is simple and efficient, and the economic advantages are obvious. Cheap synthesis gas is used as the raw material to reactwith toluene, the coupling reaction of an active intermediate for preparing methoxyaldehyde from the synthesis gas and toluene is realized in a gas-phase high-selectivity manner by adopting a fixed bed reactor under the action of the catalyst, and the preparation of high-selectivity p-methyl benzaldehyde is realized in a catalyst pore passage.