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30results about How to "Mild chemical reaction conditions" patented technology

Synthesizing method, partial intermediate products and final products of chiral beta-alkamine derivative

The invention relates to a synthesizing method, partial intermediate products and final products of a chiral beta-alkamine derivative. The synthesizing method of the chiral beta-alkamine derivative is characterized by comprising the steps of: selecting commercialized materials in the market and NH2R2 as initial materials, wherein R2 is a Cl-C6 alkyl group, a C3-C6 naphthenic base and an aryl group or an aryloxy; obtaining the intermediate products and the final products through a chemical reaction process with moderate conditions, wherein R1 and R2 are the Cl-C6 alkyl group, the C3-C6 naphthenic base and the aryl group or the aryloxy, and a chiral center is in an S or R shape. The invention has the advantages that the adopted materials are easy to obtain and at low price and can meet the requirements of large-scale production, chiral compounds are used as the initial materials, optical purity is retained in consequent reaction without finding racemization, and committed steps accord with the requirements of the current green chemistry; in addition, the invention has the advantages of simple synthesizing method, good selectivity, high yield coefficient, easy operation and good market benefits.
Owner:ASYMCHEM LIFE SCI TIANJIN

Reducing response magnetic drug-loaded nanoparticles with synergetic anti-cancer interaction and preparation method of reducing response magnetic drug-loaded nanoparticles

InactiveCN106822902AReductively responsiveSuperparamagnetic responsivenessOrganic active ingredientsPharmaceutical non-active ingredientsSide effectSuperparamagnetism
The invention relates to reducing response magnetic drug-loaded nanoparticles with synergetic anti-cancer interaction and a preparation method of the reducing response magnetic drug-loaded nanoparticles. The drug-loaded nanoparticles are prepared from a polymer prodrug and inorganic nanoparticles, which are connected through a disulfide bond; and the inorganic nanoparticles include surface-aminated superparamagnetism ferroferric oxide nanoparticles (SPION-NH2) and aminated selenium nanoparticles (NH2-R-SeNPs) employing an amino-containing high polymer as a template. The preparation method specifically comprises the following steps: (1) mixing an SPION-NH2 solution with an NH2-R-SeNPs dispersing liquid and adjusting the pH value to be 4.5-5.5; (2) dissolving the polymer prodrug connected through the disulfide bond by using ultrapure water and adjusting the pH value to be 5; and (3) dropwise adding the solution obtained in step (1) to the solution obtained in step (2), adjusting the pH value of a system to be 7.4, stirring the solution at room temperature for 10-14h to obtain the reducing response magnetic drug-loaded nanoparticles with synergetic anti-cancer interaction. The drug-loaded nanoparticles have the advantages of specific responsiveness in a targeted area, synergetic interaction and a low toxic or side effect.
Owner:WUHAN INSTITUTE OF TECHNOLOGY

Monomer for identifying halogen anions, polymer and preparation method of monomer and polymer

The invention discloses a monomer N-(p-acetenyl)-phenyl-2-X-tetrafluorobenzamide (X=F, Cl, Br and I) for identifying halogen anions, a polymer, and a method for preparing the monomer and the polymer. The method comprises the following steps: by taking 4-ethynylaniline and hexafluorobenzoic acid as main initial raw materials, taking N,N-dimethyl-4-aminopyridine as a catalyst, finally synthesizing a target small molecule compound N-(p-acetenyl)-phenyl-2-X-tetrafluorobenzamide; and by taking a precious metal complex Rh+(2,5-nbd)[(eta6-C6H5)B-(C6H5)3] (triphenyl-eta6-phenylboron-2,5-norborneol diene rhodium, Rh(nbd)BPh4) as a catalyst, thereby obtaining the poly-N-(p-acetenyl)-phenyl-2-X-tetrafluorobenzamide by virtue of a coordination polymer orientation method. The obtained small molecule monomer and polymer molecular structures simultaneously contain hydrogen bond donors and halogen bond donors, and the monomer and polymer can identify the halogen anions by virtue of coordination of hydrogen bonds and halogen bonds. Meanwhile, the preparation method has the advantages of the reaction conditions are mild, the reaction process is simple, the method is easy to control, the yield of the obtained product is high and the like.
Owner:TIANSHUI NORMAL UNIV

Monomer with anion recognizing function, oligomer and preparation method thereof

The invention discloses a N-p-nitrophenyl-N-(p-acetenyl-2-pentafluorobenzoic acid benzoyloxycarbonyl)-phenyl-urea monomer, an oligomer and a preparation method thereof. As a target product of the technology, the N-p-nitrophenyl-N-(p-acetenyl-2-pentafluorobenzoic acid benzoyloxycarbonyl)-phenyl-urea and the oligomer structure have urea structure units which can be used as hydrogen-bond donors, also have aromatic-ring structure units which can be used as anion-n donors, and when the urea structure units and the aromatic-ring structure units are combined with the anions, the synergy on the space geometry is achieved, i.e., the N-p-nitrophenyl-N-(p-acetenyl-2-pentafluorobenzoic acid benzoyloxycarbonyl)-phenyl-urea can recognize anions by the synergistic effect of two weak bonds such as hydrogen bonds and anion-n simultaneously, the target-product oligomer of the N-p-nitrophenyl-N-(p-acetenyl-2-pentafluorobenzoic acid benzoyloxycarbonyl)-phenyl-urea has the same space geometrical structure with the monomer thereof, i.e., a plurality of anions also can be recognized and combined by the synergistic effect of the two weak bonds such as the hydrogen bonds and the anion-n.
Owner:TIANSHUI NORMAL UNIV

Method for preparing ticagrelor solution

The invention discloses a method for preparing a ticagrelor solution. According to the invention, hydroxy of a ticagrelor I crude product is protected by a protective group, then a crude product of a compound II is separated and purified to obtain the high purity compound II; the hydroxy protective group of the high purity compound II is removed under proper reaction conditions, a reaction mixture is post-processed and then the by-product is removed to obtain the high purity ticagrelor I, the ticagrelor I, a solvent or / and pharmaceutic adjuvant form a solution, after the solvent is removed, ticagrelor or a mixture containing ticagrelor and accessory with medicinal requirement can be obtained. The method has the advantages of mild reaction condition, simple operation, low cost, and environmental protection, and is suitable for industrial production.
Owner:SHANGHAI FANGNAN PHARMA

Sulfated polyacrylate emulsion and preparation method thereof

PendingCN114195932ALarge total concentrationHigh total concentrationMicrosphereReaction temperature
The invention provides a preparation method of sulfated polyacrylate emulsion, which comprises the following steps: activating polyacrylate-based spheres, carrying out two-time bonding reaction on the activated microspheres, and carrying out repeated cleaning and solution washing treatment to finally obtain the sulfated polyacrylate emulsion. According to the preparation method, reaction is carried out in a water phase system, the reaction temperature is mild, and the pressure is close to normal pressure, so that reaction condition control is easily realized; the sulfated polyacrylate emulsion obtained through the preparation method is uniform in particle size, the particle size ranges from 15 micrometers to 90 micrometers, the pore diameter is as follows: the sulfated polyacrylate emulsion has better hydrophilicity, non-specific adsorption with biological samples is avoided to the maximum extent, compared with other hydrophobic filler, the pore diameter is larger, and the hydrophobicity is better than that of other hydrophobic filler. The method is more suitable for separation and purification of biological samples with larger molecular weight; meanwhile, the preparation method is simple in process, and the used raw materials are easy to obtain, so that the production cost is low.
Owner:赛分科技扬州有限公司

A kind of preparation method of doripenem

The invention belongs to the field of medicine synthesis and particularly relates to a doripenem preparation method. The method includes the steps that a compound 5 reacts with concentrated sulfuric acid in methanol to obtain a compound 4; the compound 4 and p-Nitrobenzyl-6-(1-hydroxyethyl)-1-azabicyclo(3.2.0)heptane-3,7-dione-2-carboxylate (a compound 3) are subjected to a condensation reaction under the condition that N,N-diisopropylethylamine exists, water and ethyl acetate are added and stirred after the reaction, an ethyl acetate layer is collected, alcohol is added in ethyl acetate collection liquid, crystallization is carried out, and a compound 2 is obtained; the product is dissolved through ethyl acetate; after a monopotassium phosphate solution and a phase transfer reagent of triethylbenzylammonium chloride are added, zinc powder is added into the ethyl acetate / monopotassium phosphate solution in batches to react and obtain doripenem. According to the method, reaction conditions are moderate, the technology is simple, and the conversion rate and the yield are high. Two-phase reaction is used in deprotection reaction, and the after-treatment process is simplified. The zinc powder which is cheap is used, so that the method is economical, and a new concept and a new method are provided for doripenem preparation.
Owner:SHANDONG LUOXIN PHARMA GRP CO LTD

Polyacrylate-based ball and amine salt modification method thereof

The invention provides an amine salt modification method for polyacrylate-based balls, which comprises the following steps: carrying out bonding reaction on activated polyacrylate-based balls, and carrying out repeated cleaning and solution washing treatment to finally obtain a polyacrylate emulsion. According to the amine salt modification method, the reaction is carried out in a water phase system, the reaction temperature is mild, the pressure is close to normal pressure, so that the reaction condition control is easily realized, the particle size of the obtained emulsion is 15-90 microns, the pore diameter is that the polyacrylate emulsion has better hydrophilicity, non-specific adsorption with biological samples is avoided to the greatest extent, and the application prospect is wide. Compared with other hydrophobic fillers, the hydrophobic filler has larger pore diameter and is more suitable for separation and purification of biological samples with larger molecular weight; meanwhile, the amine salt modification method is simple in process, and the used raw materials are easy to obtain, so that the production cost is relatively low.
Owner:赛分科技扬州有限公司

Monomers and polymers for recognition of halide anions and methods of preparation

The invention discloses a monomer N-(p-acetenyl)-phenyl-2-X-tetrafluorobenzamide (X=F, Cl, Br and I) for identifying halogen anions, a polymer, and a method for preparing the monomer and the polymer. The method comprises the following steps: by taking 4-ethynylaniline and hexafluorobenzoic acid as main initial raw materials, taking N,N-dimethyl-4-aminopyridine as a catalyst, finally synthesizing a target small molecule compound N-(p-acetenyl)-phenyl-2-X-tetrafluorobenzamide; and by taking a precious metal complex Rh+(2,5-nbd)[(eta6-C6H5)B-(C6H5)3] (triphenyl-eta6-phenylboron-2,5-norborneol diene rhodium, Rh(nbd)BPh4) as a catalyst, thereby obtaining the poly-N-(p-acetenyl)-phenyl-2-X-tetrafluorobenzamide by virtue of a coordination polymer orientation method. The obtained small molecule monomer and polymer molecular structures simultaneously contain hydrogen bond donors and halogen bond donors, and the monomer and polymer can identify the halogen anions by virtue of coordination of hydrogen bonds and halogen bonds. Meanwhile, the preparation method has the advantages of the reaction conditions are mild, the reaction process is simple, the method is easy to control, the yield of the obtained product is high and the like.
Owner:TIANSHUI NORMAL UNIV

Vildagliptin preparation method

The invention discloses a vildagliptin preparation method, and relates to the technical field of preparation of pyrrolidine heterocyclic compounds. The method comprises the following steps: 1, preparing an acetonitrile solution of S-1-chloroacetyl-2-cyanpyrrolidine; 2, adding acetonitrile into a reaction kettle, stirring, adding 3-amino-1-adamantanol, potassium carbonate and potassium iodide, heating, adding the acetonitrile solution of S-1-chloroacetyl-2-cyanpyrrolidine in a dropwise manner, and carrying out a heat insulation reaction after the dropwise addition until the reaction is completely carried out; and 3, post-processing: cooling, stirring, centrifuging, collecting the obtained filter cake, adding dichloromethane into the kettle, stirring, adding the filter cake, stirring, centrifuging, collecting the obtained filtrate, concentrating the filtrate to obtain a concentrate, re-crystallizing the concentrate by using isopropanol to obtain a crude product, carrying out hot washing on the crude product by using isopropanol, cooling, and centrifuging to obtain a product. The product is obtained through the one-step reaction by using the method, the yield is high, the chemical purity and the chiral purity are respectively greater than 99%, and the method has the advantages of short reaction time, low energy consumption and simple operation.
Owner:CANGZHOU SENARY CHEM SCI TEC

Synthesizing method, partial intermediate products and final products of chiral beta-alkamine derivative

The invention relates to a synthesizing method, partial intermediate products and final products of a chiral beta-alkamine derivative. The synthesizing method of the chiral beta-alkamine derivative is characterized by comprising the steps of: selecting commercialized materials in the market and NH2R2 as initial materials, wherein R2 is a Cl-C6 alkyl group, a C3-C6 naphthenic base and an aryl group or an aryloxy; obtaining the intermediate products and the final products through a chemical reaction process with moderate conditions, wherein R1 and R2 are the Cl-C6 alkyl group, the C3-C6 naphthenic base and the aryl group or the aryloxy, and a chiral center is in an S or R shape. The invention has the advantages that the adopted materials are easy to obtain and at low price and can meet the requirements of large-scale production, chiral compounds are used as the initial materials, optical purity is retained in consequent reaction without finding racemization, and committed steps accord with the requirements of the current green chemistry; in addition, the invention has the advantages of simple synthesizing method, good selectivity, high yield coefficient, easy operation and good market benefits.
Owner:ASYMCHEM LIFE SCI TIANJIN
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