44results about How to "Gentle synthesis method" patented technology

The invention provides sulfamate serving as an indoleamine-2, 3-dioxygenase inhibitor and a preparation method and application thereof. The structure of the inhibitor is shown in the general formula I, wherein definitions of X, R1, R2, R3, R4, R5 and n are shown in the description and the claim. The invention further discloses the preparation method of the inhibitor. The compound shown in the general formula I can serve as the indoleamine-2, 3-dioxygenase inhibitor and is used for preparing medicine for preventing and/or treating indoleamine-2, 3-dioxygenase mediated diseases. The general formula I is shown in the description.

The invention relates to a fasudil hydrochloride compound and a novel method thereof. The method comprises the following steps of: in the presence of a solvent, performing sulfonation reaction on a chlorosulfonic acid serving as a sulfonating agent and isoquinoline to generate a 5-isoquinolinesulfonic acid; reacting the 5-isoquinolinesulfonic acid with thionyl chloride under a heating condition to generate isoquinoline-5-sulfonyl chloride hydrochloride; and dissolving the isoquinoline-5-sulfonyl chloride hydrochloride with ice water, adjusting the pH value of the solution with sodium bicarbonate, reacting the solution with homopiperazine, adjusting the pH value again with a hydrochloric acid, and concentrating under reduced pressure and recrystallizing to prepare the fasudil hydrochloride compound. The synthesis method of the invention has the advantages of mild reaction conditions, high yield and easy industrial production.

The invention relates to an aptamer modified triazine covalent organic framework composite material and a preparation method and application thereof. The aptamer modified triazine covalent organic framework composite material disclosed by the invention comprises a triazine covalent organic framework, gold nanoparticles and an aptamer, wherein the gold nanoparticles are supported on the triazine covalent organic framework; and the aptamer is bonded onto the surface of the gold nanoparticles. When the sequence of the aptamer is 5'-SH-(CH2)6-(ACAG4TGTG4)2-3', the composite material disclosed by the invention can be applied to enrichment of insulin in biological samples. The aptamer modified triazine covalent organic framework composite material disclosed by the invention combines the advantages of the covalent organic framework such as large specific surface area and multiple adsorbable sites and the advantage of the aptamer such as specific recognition, has excellent selectivity, and canprovide an economic, high-efficiency and high-sensitivity biological analysis method.

The invention discloses a platinum complex for inhibiting cell SKOV3 and a synthesis method of the platinum complex, belongs to the technical field of medicines, and aims to provide a cell SKOV3 inhibiting platinum complex synthesized from rutaecarpine as structural basis and DMSO as an auxiliary ligand. The invention further provides a synthesis method of the platinum complex. The structural formula of the platinum complex is as shown in the description. The platinum complex can be used for preparing anti-tumor drugs.

The invention relates to targeted nanometer photosensitizer for photodynamics deep tumor therapy and a preparing method thereof. According to the preparing method, protein, or polypeptide or amino acid is used for reacting with a soluble copper salt solution, and the monovalence protein chelated targeted nanometer photosensitizer or the polypeptide-copper chelated targeted nanometer photosensitizer or the amino acid-copper chelated targeted nanometer photosensitizer is obtained after reduction. Under excitation of X rays with the dosage much lower than a general radiotherapy dosage, the targeted nanometer photosensitizer can generate strong fluorescence and has a photodynamics therapy effect on tumors. The targeted nanometer photosensitizer is small in particle size, good in water solubility, small in toxic and side effect and capable of being endocytosed by deep tumor cells easily. The X rays serve as an excitation light source of the targeted nanometer photosensitizer, the therapy efficiency is high, and the problems that existing photodynamics therapy cannot be carried out on the deep tumors, and skin phototoxicity is caused can be solved. Reaction conditions of the photosensitizer are moderate, and the photosensitizer can be industrially manufactured, achieves energy conservation and environment protection, can promote the silkworm breeding and mulberry growing industrial chain to develop in the high value-added industry direction, and has good economic benefits, social benefits and ecological benefits.

The invention provides a preparation method of a phosphate ester or a phosphite ester. The preparation method comprises the following step: reacting an inorganic phosphate or an inorganic phosphite with a silicon-substituted cycl-lactam compound shown in a formula 3) to obtain the phosphate ester shown in a formula 1) or the phosphite ester shown in a formula 2). The preparation method provided bythe invention not only can be used for preparing phosphate esters, but also can be used for preparing phosphite esters. The synthetic method disclosed by the invention is mild and stable in reaction,convenient to operate, high in yield, high in purity and low in energy consumption in the reaction process, and is a universal synthetic method for synthesizing phosphate esters or phosphite esters.

The invention belongs to the field of pharmaceutical chemistry and relates to a novel phosphoinositide 3-kinase inhibitor, a preparation method and an application thereof. Specifically, the present invention provides a compound having the structure of formula I, which can be used as an efficient PI3K inhibitor and has various pharmacological activities such as tumor resistance, resistance to neurodegenerative diseases (such as Alzheimer's disease), inflammatory resistance, etc.

The invention relates to a carbon felt-loaded cerium-doped alpha-FeOOH nanosheet array electrode, a preparation method thereof and application of the carbon felt-loaded cerium-doped alpha-FeOOH nanosheet array electrode in electro-Fenton water treatment. The preparation method comprises the following steps: firstly, preparing an aqueous solution containing an iron source and a cerium source; and adding glycerol and a conductive carbon felt, carrying out hydrothermal reaction, and carrying out post-treatment to obtain the nanosheet array electrode. The nanosheet array electrode can be used as a cathode material for removing organic pollutants through electro-Fenton reaction. Compared with the prior art, the cerium-doped alpha-FeOOH nanosheet array loaded carbon felt electrode prepared by the preparation method disclosed by the invention is simple in synthesis method, free of metal dissolution, stable in reutilization performance and high in mineralization rate, and has a wide prospect in industrial wastewater treatment.

The present invention discloses an efficient IDO/TDO double inhibitor containing a nitrogen heterocyclic helix structure, and in particular, relates to a compound of formula (I) or pharmaceutically acceptable salt, stereoisomers, or tautomers, or prodrugs thereof. The compound of the formula (I) can be used as an indoleamine-2,3-dioxygenase inhibitor and tryptophan-2,3-dioxygenase for preparationof drugs for prevention and/or treatment of indoleamine-2,3-dioxygenase and tryptophan-2,3-dioxygenase-mediated diseases.

The invention specifically relates to a biological preparation method for a photoelectric conversion material, belonging to the field of photoelectrochemistry. The biological preparation method comprises the following steps: with sulfate-reducing bacteria used as a biological material, carrying out enrichment culture in a culture solution, then adding an excess aqueous CdSO4 solution, carrying out a reaction for 30-60 minutes at room temperature, and then carrying out centrifugation and drying so as to obtain the biosynthetic photoelectric conversion material. The preparation method of the invention is simple in process, easy to operate and low in cost, and has potential application value in the research fields of photoelectrochemical solar cells, photoelectrochemical decomposition of water, photoelectrochemical analysis, etc.

The invention discloses a Fe<3+> detection hyperbranched conjugated polymer and a preparation method and application thereof. A structural unit of the polymer is as shown in the specification, wherein R refers to one of carbomethoxy, carbethoxy, tert-butoxycarbonyl, cyano, nitro and -COONa arbitrarily. By MBH-type reaction synthesis, mild reaction conditions, environment friendliness and freeness of metal catalyst residues are realized; since Fe<3+> ions have an evident quenching effect on fluorescence of a tetrahydrofuran solution or an aqueous solution of the synthesized hyperbranched conjugated polymer, the hyperbranched conjugated polymer can be used for detection of Fe<3+> ions in an aqueous phase or an organic phase and is high in Fe<3+> ion selectivity and low in Fe<3+> ion detection limit.

The invention relates to a preparation method of a CDKs inhibitor of a beta-carboline parent nucleus and an anti-tumor application of the CDKs inhibitor, and particularly provides a novel beta-carboline derivative with CDKs inhibition activity, an application of the novel beta-carboline derivative in anti-tumor, and a preparation method of the compound. The synthesis method is simple and mild; the compound disclosed by the invention can effectively inhibit CDK4, and has the activities of resisting tumor cell proliferation activity, inhibiting tumor cell migration and invasion, inducing tumor cell apoptosis, inhibiting nude mouse subcutaneous tumor-bearing growth and the like. Therefore, the compound as a lead compound plays an important role in tumor treatment.

The invention relates to a preparation method of a hierarchical porous metal organic framework chiral sensing probe, which comprises the following steps of providing a hierarchical porous metal organic framework microsphere with a regular pore structure, fixing amino acid oxidase on the hierarchical porous metal organic framework microspheres to obtain hierarchical porous metal organic framework microspheres fixed with enzymes, and loading the amino acid oxidase in pore channels of the hierarchical porous metal organic framework microspheres through adsorption, fixing fluorescent molecules on the hierarchical porous metal organic framework microspheres fixed with enzyme to obtain the hierarchical porous metal organic framework chiral sensing probe, and loading the fluorescent molecules in pore channels of the hierarchical porous metal organic framework microspheres through adsorption. The invention also provides the hierarchical porous metal organic framework chiral sensing probe obtained by the preparation method and application thereof. By fixing different amino acid oxidase as a chiral recognition center, the amino acid can be recognized and the content of the amino acid can be analyzed in a high-sensitivity and high-specificity manner.

The invention discloses a synthesis method of a cabozantinib dimer. The method comprises the following steps: preparation of 4-chloro-6,7-dimethoxyquinoline, preparation of an intermediate 1, and preparation of a cabozantinib dimer impurity; and preparation of cabozantinib dimer impurities: adding an organic solvent into a reactor at room temperature, stirring for 10 min, adding cyclopropanedicarboxylic acid, stirring for 20 min, then adding an intermediate 1 with the mass ratio of the intermediate 1 to the cyclopropanedicarboxylic acid being 400:115, carrying out a reaction for 3 h, enablingthe raw material to remain 4%, heating to 45 DEG C until the reaction is complete, adding water, separating out the product, and carrying out suction filtration to obtain the cabozantinib dimer impurities. By adopting the synthesis method of the cabozantinib dimer, no high-temperature and high-pressure reaction exists in the synthesis process, the synthesis method is mild and easy to operate, allthe steps are mild and controllable, the operation is simple, and the controllability is high.

The invention discloses a rutaecarpine alkali gold salt as well as a synthesis method and an application thereof, belongs to the technical field of medicines and aims to provide the rutaecarpine alkali gold salt, the synthesis method thereof and the novel application of the rutaecarpine alkali gold salt in the antitumor field. The structural formula of the rutaecarpine alkali gold salt is as shown in the description. The rutaecarpine alkali gold salt can be used for preparing an antitumor medicine.