38 results about "Aminothiazole" patented technology

The invention relates to the technical field of corrosion inhibitors in the pickling industry, in particular to a preparation method and application of a Mannich base thiadiazole quaternary ammonium salt corrosion inhibitor for methanesulfonic acid pickling. According to the method, amino thiadiazole is modified by Mannich, quaternization is further performed, and the thiadiazole corrosion inhibitor with the advantages of Mannich base and quaternary ammonium salt is obtained. Quaternary ammonium salt groups in corrosion inhibitor molecules endow the corrosion inhibitor with good water solubility, and the dispersity and adsorbability of the corrosion inhibitor in an acid solution are improved; thiadiazole ring, thioamide and the like contained in the corrosion inhibitor contain N and S atom groups, so that coordination with metal is facilitated, and the adsorption performance of the corrosion inhibitor is improved; and the tail alkyl chain can effectively isolate corrosive substances from being in contact with a metal matrix. The preparation method is simple in synthesis step and low in raw material cost, and the obtained corrosion inhibitor is excellent in corrosion inhibition effect. Under the condition of 353 K, the highest corrosion inhibitor efficiency on Q235 steel in methanesulfonic acid with the molar concentration of 0.5 M reaches 99.8%.

The present invention covers aminothiazole compounds of general formula (I), in which R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and / or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGKζ) regulated disorders, as a sole agent or in combination with other active ingredients.

The invention relates to the technical field of detection, and particularly discloses a method for detecting 2-aminothiazole in marine sediments in a sea area near an offshore wind field, which comprises the following steps: extracting a sample by using a mixed solution, then deriving by using hexyl chloroformate, converting a target compound 2-aminothiazole into N-(thiazole-2-yl) carbamic acid n-hexyl ester, and detecting the 2-aminothiazole in the marine sediments in the sea area near the offshore wind field by using the N-(thiazole-2-yl) carbamic acid n-hexyl ester. And enriching and purifying the obtained derivative by using a solid-phase extraction small column, and detecting by using a liquid chromatography-mass spectrometry system. The method provided by the invention can be used for efficiently, quickly and accurately analyzing and detecting, and is suitable for detecting 2-aminothiazole in marine sediments.

The application discloses isobutyryl amino thiazyl resorcinol dipalmitate and a preparation method and application thereof. The compound is successfully prepared by performing an acylation reaction on isobutyryl amino thiazyl resorcinol and palmitic acid. Experiments prove that, compared with the prior art, the compound not only retains excellent whitening efficacy, but also exhibits extremely low cytotoxicity and significant soothing efficacy. The compound has whitening, soothing and high safety, overcomes the defect that traditional whitening agents are strong in irritation, and can be directly applied to cosmetics or skin external drugs, and has extremely high industrial value.

This invention relates to a flash etching solution, its preparation method, and its application. The flash etching solution comprises hydrogen peroxide, sulfuric acid, a corrosion inhibitor, a stabilizer, and water; the corrosion inhibitor comprises a combination of aminotetrazole, hydroxyethyl ethylenediaminetriacetic acid, and 2-aminothiazole. The flash etching solution provided by this invention significantly improves the stability of hydrogen peroxide, greatly extending its service life; and effectively improves problems such as large lateral corrosion and high roughness, thereby improving production efficiency and reducing production costs.

The invention discloses a high-strength modified polypropylene composite material and a preparation process thereof, and relates to the technical field of polypropylene composite materials. The high-strength modified polypropylene composite material comprises the following raw materials in parts by weight: 60-70 parts of polypropylene, 15-18 parts of modified glass fibers and 5-6 parts of a thiazolyl phosphorus-containing flame retardant. The preparation method comprises the following steps: sequentially reacting phosphorus oxychloride with p-hydroxybenzaldehyde and 2-aminothiazole to obtain a thiazolyl phosphorus-containing flame retardant; the preparation method comprises the following steps: sequentially reacting glass fibers with 3-chloropropyltriethoxysilane and tetraethylenepentamine to prepare aminated glass fibers; and carrying out a reaction on the aminated glass fiber, acrylate-based hindered phenol and 2-[3-(2H-benzotriazole-2-yl)-4-hydroxyphenyl] ethyl 2-methacrylate to prepare the modified glass fiber. The modified glass fiber and the thiazolyl phosphorus-containing flame retardant are added into polypropylene, so that the polypropylene composite material is endowed with excellent flame retardance, weather resistance and mechanical properties.

The invention relates to the technical field of anti-tumor pharmacy. Specifically, the invention relates to an anti-tumor activity application of a compound with a structure as shown in a formula I. In-vitro MTT (3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor activity evaluation finds that the compound shown in the formula I has a remarkable inhibiting effect on the growth of human colorectal cancer HCT116 and human breast cancer cells MCF-7. The anti-tumor activity of the compound with the structure shown in the formula I is disclosed for the first time, and the compound can be used for preparing medicines for resisting colorectal cancer and other tumors and has good development and application prospects. .

The present application relates to the technical field of electrocatalytic material, disclose a kind of preparation method and device of cobalt-doped nano-zinc sulfide oxygen reduction electrocatalytic material, comprising: amino thiazole, anhydrous zinc acetate and the solution of the preset concentration of cobalt nitrate hexahydrate are placed in grinding mortar and mixed grinding and drying, obtain electrocatalytic precursor, after grinding electrocatalytic precursor is placed in porcelain boat and using tube furnace to the pyrolysis precursor to be pyrolyzed, obtain pyrolysis product, using hydrochloric acid to the pyrolysis product is etched, obtain pyrolysis etching product, to pyrolysis etching product is washed and filtered, obtain initial oxygen reduction electrocatalytic material, the initial electrocatalytic product is dried, obtain target oxygen reduction electrocatalytic material.The present application is mainly aimed at solving the problem of current Pt / C catalyst with high price and low catalytic performance.

This disclosure relates to the crystalline hydrate forms of (S)-2-((R)-6-(N-((1s,3S)-3-amino-cyclobutyl)carbamimidoyl)chroman-2-yl)-2-((((Z)-1-(2-aminothiazol-4-yl)-2-(((S)-2,2-dimethyl-4-oxo-1-(sulfooxy)azetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)propanoic acid, including crystalline hydrate form A, crystalline hydrate form B and crystalline hydrate form D, which are useful as antibiotic agents for the treatment of bacterial infections, such as bacterial infections caused by gram-negative bacteria, including strains that are multidrug resistant.

The invention belongs to the technical field of medicine synthesis, and discloses a synthesis method of ceftazidime, which comprises the following steps: (1) under the action of an acid-binding agent, carrying out condensation reaction on 7-APCA and alpha-(2-aminothiazole-4-yl)-alpha-[(tert-butyloxycarboryl) isopropoxyimino] acetic acid mercaptobenzene isothiazole ester in a solvent to obtain 7-APCA-alpha (2-aminothiazole-4-yl)-alpha-[(tert-butyloxycarboryl) isopropoxyimino] acetic acid mercaptobenzene isothiazole ester; after the reaction is finished, carrying out post-treatment to obtain ceftazidime tert-butyl ester; in the step (1), the acid-binding agent is isooctylamine and an aniline compound in a mass ratio of (1-5): 1; (2) hydrolyzing and crystallizing the ceftazidime tert-butyl ester obtained in the step (1) under an acidic condition to obtain ceftazidime hydrochloride; and (3) further neutralizing and crystallizing the ceftazidime hydrochloride in the step (2) to obtain the ceftazidime. According to the synthesis method, by adopting the composite acid-binding agent, side reactions are reduced, the content of by-products is reduced, and the purity of the product is improved.

The present invention relates to extended release composition of Mirabegron and process of manufacture thereof. The extended release composition of mirabegron comprising non-polymeric hydrophobic excipient as release controlling agent along with one or more pharmaceutically acceptable excipient is used in the treatment of symptoms associated with overactive bladder.

The application discloses a kind of synthesis method of dasatinib intermediate in the field of organic synthesis, with 2-aminothiazole-4-carboxylic acid as raw material, first and tert-pivaloyl chloride in situ generates mixed anhydride, further and 2-chloro-6-methylaniline condensation reaction occurs after, the compound 2 obtained is not separated directly hydrolyzed to obtain high-purity 2-amino-N-(2-chloro-6-methylphenyl) thiazole-5-formamide.Due to the mixed anhydride formed by tert-pivaloyl chloride has greater steric hindrance, and the further reaction of corresponding amine is conducive to the regioselectivity, and by-product tert-pivalic acid can be easily removed by post-treatment, so as to solve the disadvantages existing in the prior art, the unit operation involved in the whole preparation process is simpler, and the product purity and yield are higher, with good application prospect.

The invention belongs to the technical field of chemical synthesis, and discloses a cefotaxime sodium synthesis method based on one-step salification of a mixed solvent system and sodium isooctanoate. The method comprises the following steps: by taking 7-aminocephalosporanic acid (7-ACA) and 2-(2-aminothiazole-4-yl)-2-(methoxyimino) acetoxyimino ethyl acetate (AE active ester) as raw materials, in a dichloromethane-methanol mixed solvent, completing a condensation reaction through triethylamine catalysis, directly dropwise adding a sodium isooctanoate acetone solution to realize salification in one step, and carrying out post-treatment to obtain the 7-aminocephalosporanic acid (7-ACA)-2-(methoxyimino) acetoxyimino ethyl acetate (AE active ester)-2-(methoxyimino) acetoxyimino ethyl acetate (AE active ester). The cefotaxime acid intermediate does not need to be separated; and performing low-temperature washing and accurate drying subsequently to obtain a cefotaxime sodium finished product. According to the method, the defects that in the prior art, a two-step method needs intermediate separation and a one-pot method needs alkaline degradation are overcome, the production period is shortened to be smaller than or equal to 8 h, the total yield is larger than or equal to 92%, the HPLC purity is larger than or equal to 99.6%, the wastewater COD is smaller than or equal to 2000 mg / L, solvent residues meet the ICH Q3C standard, and the method has the advantages of industrial feasibility and environmental protection.

The invention provides a pyridone-containing aminothiazole heterocyclic compound as well as synthesis and application thereof. The aminothiazole heterocyclic compound has a structure as shown in a general formula I or a general formula II or a pharmaceutically acceptable salt or an isotope labeled compound thereof. The invention also discloses a preparation method and the like of the derivative. Experiments prove that the aminothiazole heterocyclic compound containing pyridone can effectively inhibit replication of herpes simplex virus in Vero cells, the compound is of a non-nucleoside structure, the inhibitory activity of the compound is superior to that of a clinical first-line drug acyclovir, and the compound can be used for preparing active drugs for resisting the herpes simplex virus. The general formula I or the general formula II is shown in the specification.

(2-((1H-pyrrolo[2,3-b]pyridine-3-carbonyl)imino)-2,3-dihydrothiazol-4-yl)methyl dihydrogen phosphates and (2-((1H-pyrrolo[2,3-b]pyridine-3-carbonyl)imino)thiazolidin-4-yl)methyl dihydrogen phosphates are disclosed. The compounds activate Yap and inhibit Lats kinases. They are therefore useful for treating hearing loss.

Provided is a novel compound that exhibits an excellent control effect against harmful plant diseases. An N-substituted oxy-2-aminothiazolecarboxamide compound represented by the following formula (in the formula, each symbol is as described in the description) or a salt thereof exhibits an excellent control effect against harmful plant diseases.

The application relates to a preparation method of 2-acylaminothiazole compounds, in particular to a preparation method of an intermediate of alvocidib, in the preparation method, a mixed solution of tetrahydrofuran and DMSO is used as a solvent to form a homogeneous system, so that the preparation method has the advantages of simple post-treatment, high yield and high product purity, and the method is especially suitable for industrial production.

The present disclosure provides a novel salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide and a method for preparing the same. The mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide, which may be prepared using methanesulfonic acid and, without wishing to be bound by theory, can exhibit reduced hygroscopicity and improved physicochemical stability and solubility. In some aspects, the present disclosure provides a pharmaceutical composition for preventing or treating a sodium channel blocker-related disease, comprising the mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide.

The invention discloses an application of a 2-aminothiazole derivative in preparation of an anti-aging drug. The 2-aminothiazole derivative can effectively relieve senescence of microglial cells in vitro, reduce accumulation of senescence-related beta-galactosidase in senescence cells, reduce secretion of senescence-related secretion phenotypes and improve senescence cell apoptosis and oxidative stress loss. In a mouse in-vivo experiment, the compounds A1-A10 can remarkably improve cognitive impairment and long-term and short-term learning and memory ability damage caused by aging, reduce the transcription expression level of proinflammatory factors in the brain and relieve neuroinflammation. In conclusion, the 2-aminothiazole derivative provided by the inventor has a good anti-aging curative effect and has huge application potential in the anti-aging aspect.

Disclosed in the present invention is a use of a 2-aminothiazole derivative in the preparation of an anti-aging drug. The 2-aminothiazole derivative can effectively alleviate microglial cell aging in vitro, reduce accumulation of senescence-associated β-galactosidase in aged cells, decrease secretion of a senescence-associated secretory phenotype, and ameliorate apoptosis and oxidative stress damage in the aged cells. In a mouse in vivo experiment, compounds A1-A10 can significantly improve aging-induced cognitive dysfunction and impairment of long-term and short-term learning and memory abilities, reduce transcriptional expression levels of pro-inflammatory factors in the brain, and alleviate neuroinflammation. In summary, the present inventors propose that 2-aminothiazole derivatives have good anti-aging efficacy and possess great application potential in anti-aging.

Nano-entity compositions composed of a plurality of self-associated compounds of Formula 1 and / or Formula 2, for example, 2-[(Z)-[l-(2-amino-l,3-thiazol-4-yl)-2-oxo-2-(2-oxoethylamino)ethylidene]amino]oxyacetic acid, where R1 is a carboxylic acid group and R2 is an amine group, have antifibrotic properties, effective for inhibiting type I collagen synthesis by inhibiting binding of LARP6 with a 5' stem-loop of a collagen mRNA. The described nano-entity compositions may be used in a method of treating a patient having a fibrotic condition, including but are not limited to a pulmonary fibrosis, a liver fibrosis, a heart fibrosis, a circulatory system fibrosis, a skin fibrosis, a renal fibrosis, and / or an intestinal fibrosis.

To provide a new compound with excellent control effects against harmful plant diseases. An N-substituted oxy-2-aminothiazolcarboxamide compound represented by formula (I) or a salt thereof: wherein the reference symbols are those defined in the specification, has excellent control effects against harmful plant diseases.

microbicidal 2-acylamino-thiazol-4-carboxamide derivatives. compounds of formula (i) (i) wherein the substituents are as defined in claim 1, useful as pesticides and especially fungicides.

The invention relates to the technical field of medicine synthesis, in particular to a synthesis method and application of a 2-(3, 4-dimethoxybenzamido) thiazole-4-amide derivative. The structure of the thiazole is as shown in a formula I in the specification. The preparation method of the 2-(3, 4-dimethoxybenzamido) thiazole-4-amide derivative comprises the following step: reacting a compound shown in a formula I with a compound shown in a formula II in the presence of HATU, DIPEA, primary amine or secondary amine and tetrahydrofuran to obtain the 2-(3, 4-dimethoxybenzamido) thiazole-4-amide derivative. The 2-(3, 4-dimethoxybenzoylamino) thiazole-4-amide derivative disclosed by the invention has a relatively good effect of relieving the Alzheimer's disease, and is characterized by having relatively strong cholinesterase inhibitory activity.

The invention discloses an aminothiazole compound and an application thereof as an androgen receptor antagonist. The aminothiazole compound comprises pharmaceutically acceptable salts, solvates, prodrugs and isomers of the aminothiazole compound, and pharmaceutical compositions containing the aminothiazole compound and the pharmaceutically acceptable salts, the solvates, the prodrugs and the isomers of the aminothiazole compound. The aminothiazole compound has obvious antagonistic activity to AR, shows better biological activity in in-vivo and in-vitro biological evaluation, and is effective to an enzalutamide drug-resistant ARF876L / T877A two-point mutation model and a comparison caralutamide drug-resistant ARW741C mutant cell model. The percutaneous administration also shows the effect of promoting hair growth on a mouse alopecia model. Therefore, the compound can be used as an AR antagonist to prepare drugs for treating diseases related to androgen receptors, such as prostate cancer, metastatic prostate cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, androgen-derived alopecia and acne.

The application discloses a preparation method of concentration-dependent red light sulfur quantum dots and the red light sulfur quantum dots. The preparation method comprises the following steps: grinding, and reacting with sublimed sulfur, inorganic alkali and a heterocyclic functional reagent as raw materials and hydrogen peroxide as an etching agent; and then performing dialysis and freeze-drying to obtain the red light sulfur quantum dots. The heterocyclic functional reagent is a nitrogen-containing heterocyclic compound, and is at least one of 2-aminothiazole, imidazole-2-formaldehyde and 2-aminooxazole. The three SQDs all have concentration dependence, and the optimal emission wavelength is gradually red-shifted with the increase of the SQD concentration, and the maximum red shift is 130 nm. The maximum emission wavelength of the prepared SQDs can reach 690 nm, which indicates that the SQDs are red light emission fluorescent nanomaterials, and the fluorescence wavelength red shift can be attributed to non-radiative transition due to molecular assembly at a high concentration, i.e. fluorescence resonance energy transfer, and production of new emission centers. The application provides a new strategy for the research of concentration-dependent nanomaterials and red light emission SQDs.

Embodiments of the present disclosure pertain to methods of conjugating a molecule to a polypeptide by (1) modifying one or more thiol residues on the polypeptide, where the modifying includes cyanylation of the one or more thiol residues; and (2) associating the polypeptide with the molecule, where the associating results in the conjugation of the molecule to the polypeptide through a reaction between a nucleophilic moiety on the molecule and the one or more modified thiol residues. The cyanylation may include attachment of cyano groups to sulfur atoms of the one or more thiol residues to form thiocyanato groups that undergo reversible intramolecular addition with a nearby N-amide group to generate a 1-acyl-2-iminothiazolidine intermediate. Thereafter, the nucleophilic moiety on the molecule reacts with the 1-acyl-2-iminothiazolidine intermediate to replace 2-iminothiazolidine in a nucleophilic acyl substitution reaction and result in the conjugation of the molecule to the polypeptide.

The invention provides disperse blue 360 and a preparation method thereof. The preparation method comprises the following steps: a diazotization step: under an acidic condition, carrying out a diazotization reaction on 2-aminothiazole and a diazotization reagent to obtain a diazonium solution; a coupling step: carrying out a coupling reaction on N, N-diethyl m-toluidine and the diazonium liquid to obtain a coupling product; nitration: carrying out nitration reaction on the coupling product and nitric acid to obtain a nitration product containing disperse blue 360. The preparation method disclosed by the invention is simple and easy to implement, the stability of the coupled material is remarkably improved, and the decomposition loss of the raw material in the nitration process of the 2-aminothiazole is effectively reduced. The preparation method disclosed by the invention can greatly improve the yield of the product and remarkably save the production cost, and is suitable for large-batch production.