27 results about "Benzothiazine" patented technology

The invention discloses a benzothiazine phenothiazine oxide polyacrylamide copolymer phosphorescent material as well as a preparation method and application thereof, belongs to the technical field of organic phosphorescent materials, and solves the problems of harsh ORTP preparation conditions and unsatisfactory product performance in the prior art. The room-temperature phosphorescent material is obtained mainly by introducing different connecting units to the benzothiazine phenothiazine oxide and then carrying out free radical copolymerization with acrylamide, the reaction conditions are mild, the synthesis method is simple and convenient, and the materials are easy to obtain.

The present invention belongs to the field of medicine and relates to the use of benzothiazinone vinylidene indene compounds in the preparation of osteoclast differentiation inhibitors. The present invention uses tartrate-resistant acid phosphatase (TRAP) staining and reverse transcription real-time fluorescence quantitative polymerase chain reaction (RT-qPCR) technology to confirm for the first time that this series of compounds can significantly inhibit RANKL-induced osteoclast differentiation and the formation of multinucleated osteoclasts, and are non-cytotoxic at concentrations of 5μM and below. Based on these findings, the benzothiazinone vinylidene indene compounds provided by the present invention can be used as candidate drug molecules for novel osteoclast differentiation inhibitors, for the prevention and / or treatment of bone metabolic diseases caused by excessive activation of osteoclasts, such as osteoporosis, periprosthetic bone dissolution, tumor metastasis bone destruction, and rheumatoid arthritis.

The present invention is directed to dihydroquinazoline, -benzothiazine and -benzoxazine derivatives, advantageously for use in the prevention or treatment of neurological, psychiatric and sleep disorders and diseases in which central orexin neurotransmission is impaired or in which central and peripheral orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds for use in the prevention and / or treatment of neurological disorders and diseases. The present invention is also directed to dihydroquinazoline, -benzothiazine and -benzoxazine derivatives and the use of these compounds as medicaments.

The invention relates to the technical field of compound synthesis and pesticides, in particular to benzothiazinone pyrazole derivatives as well as a preparation method and application thereof, and the general formula of the benzothiazinone pyrazole derivatives is as shown in formula I; the derivative has effective pre-emergence and post-emergence herbicidal activity, is high in safety to crops and can be applied to preparation of herbicides; the derivative is simple in structure and preparation process, low in production cost and wide in application prospect.

The application relates to the fine chemical technology field and discloses a preparation method of 2-substituted-2,3-dihydro-4 H benzothiazine-4-ketone. The specific steps are as follows: 1,2-benzisothiazolin-3-ketone and carbonyl compound are used as raw materials, hydrogen iodide and ammonium iodide are used as important additives, one-step reaction is carried out in an organic solvent, and the target product can be obtained after purification. The method is simple in operation, high in yield and has potential application value.

The invention belongs to the field of chemical pesticides, and relates to an insecticide, in particular to benzo [e] [1, 3] thiazine-2, 4-diketone compounds, pharmaceutically acceptable salts and a preparation method thereof.The benzo [e] [1, 3] thiazine-2, 4-diketone compounds are prepared by stirring benzo [c] [1, 2] dithio-3-ketone compounds and triphenylphosphine in a solvent and then adding carbamic acid p-nitrophenyl ester compounds for a synthetic reaction. The compound is a 3, 3] thiazine-2, 4-diketone compound. Compared with a traditional synthesis method, the method has the advantages that raw materials are easy to prepare, the highest yield can reach 99%, reaction conditions are mild, operation is easy and the like, it is found through insecticidal activity screening that the synthesized benzo [e] [1, 3] thiazine-2, 4-diketone compound has good insecticidal activity, and the method has important significance on research of synthesis and application of the compound.

The present application relates to the technical field of organic synthesis, and particularly relates to a method for synthesizing 3-methyl-2-phenyl-2,3-dihydrobenzothiazine-4-ketone. A conventional method for synthesizing 3-methyl-2-phenyl-2,3-dihydrobenzothiazine-4-ketone generally uses anthranilic acid as a starting material, and needs to be subjected to six-step continuous reactions to obtain the product, and the reaction time is long, the yield is low, and the operation is complicated. In view of the above problems, the present application provides a method for synthesizing 3-methyl-2-phenyl-2,3-dihydrobenzothiazine-4-ketone, which uses 2-mercapto-N-methyl benzamide as a starting material, and is completed through one-step reaction, and the starting material and catalyst are easy to obtain, the operation is simple, the reaction is fast, the equipment requirement is low, the post-treatment is simple, and the yield is high.

The application provides a milk exosome coated PLGA nanometer anti-tuberculosis drug system and preparation and application. The system structure is: anti-tuberculosis drug-milk exosome@PLGA-anti-tuberculosis drug. The anti-tuberculosis drug is selected from a combination of one or more of aminoquinolones, benzothiazoles, arylquinolines, nitrobenzamide and benzothiazinone anti-tuberculosis drugs. The nanometer anti-tuberculosis drug system prolongs the circulation time of nanoparticles in blood, improves the bioavailability of the drug, enhances the cell uptake efficiency of nanoparticles, improves the drug delivery effect, reduces the immune rejection reaction and potential toxicity, and improves the safety of treatment.

The present invention relates to dihydroquinazoline, dihydrobenzothiazine and dihydrobenzoxazine derivatives for use in the prevention or treatment of neurological, psychiatric, sleep disorders and diseases, advantageously in which central orexin neurotransmission is impaired or in which central and peripheral orexin receptors are involved. The invention also relates to pharmaceutical compositions comprising these compounds, their use for the prevention and / or treatment of nervous system disorders and diseases. The invention also relates to dihydroquinazoline, dihydrobenzothiazine and dihydrobenzoxazine derivatives, and to the use of these compounds as medicaments.

The invention belongs to the technical field of medicines, and particularly relates to an aryl alkyl azole derivative as well as a preparation method and application thereof. Benzo [d] [1, 3] thiazine is used as aryl and is directly connected with 4H-1, 2, 4-triazole-4-yl through a chemical bond, and alkoxy is introduced to the C6 position of the aryl, so that the aryl alkyl azole derivative is obtained. The compound disclosed by the invention is novel in structure, shows excellent anti-convulsion activity in two epilepsy models of maximum electroshock and subcutaneous pentyltetrazole as a GABAA receptor agonist, and particularly shows an extremely high protection index, PIgt, in the subcutaneous pentyltetrazole model; and 10, the compound has the remarkable advantages of various action mechanisms, wide therapeutic window and low neurotoxicity, can be used for preparing the anti-epilepsy medicine, and is particularly suitable for treating intractable epilepsy.

The invention relates to the technical field of organic synthesis, in particular to a method for synthesizing N-(acetamidomethyl) benzothiazine-4-ketone. At present, N-chloromethylacetamide is used in a synthetic method of N-(acetamidomethyl) benzothiazine-4-ketone, the synthetic route of the N-chloromethylacetamide is complex, and toxic raw materials such as CO gas also need to be used in the synthetic process of the N-chloromethylacetamide. In order to solve the problems, the invention provides the method for synthesizing the N-(acetamidomethyl) benzothiazine-4-ketone, the N-(acetamidomethyl) benzothiazine-4-ketone is successfully prepared by taking benzothiazine-4-ketone, DABCO.DCM, hydroiodic acid, acetonitrile and the like as reaction raw materials through a one-pot method, the use of N-halogenated methylacetamide is avoided in the reaction, and the reaction yield is high. The reaction is more efficient, and the reaction process is more environment-friendly.

The invention belongs to the field of medicines, and relates to application of a benzothiazinone vinylidene indene compound in preparation of an osteoclast differentiation inhibitor. Through tartrate-resistant acid phosphatase (TRAP) staining and reverse transcription real-time fluorescent quantitative polymerase chain reaction (RT-qPCR) technologies, it is proved for the first time that the series of compounds can significantly inhibit RANKL-induced osteoclast differentiation and polykaryotic osteoclast formation, and have no cytotoxicity at the concentration of 5 [mu] M or below. Based on the discoveries, the benzothiazinone vinylidene indene compound provided by the invention can be used as a candidate drug molecule of a novel osteoclast differentiation inhibitor, and is used for preventing and / or treating osteoporosis, periprosthetic osteolysis, tumor metastasis bone destruction, rheumatoid arthritis and other bone metabolism diseases caused by overactivity of osteoclasts.

The invention relates to a preparation method of 4 '-chloro-2-aminobiphenyl, and relates to the technical field of organic synthesis.The preparation method comprises the following steps that p-dichlorobenzene, a sulfur trioxide-pyridine compound and thionyl chloride are subjected to a reaction, and 2, 5-dichlorobenzene sulfonyl chloride is obtained; the preparation method comprises the following steps: reacting 2, 5-dichlorobenzenesulfonyl chloride, aniline hydrochloride and a sodium bicarbonate solution to obtain 2, 5-dichloro-N-phenylbenzenesulfonamide; the preparation method comprises the following steps: reacting 2, 5-dichloro-N-phenylbenzenesulfonamide, cysteine, a titanium dioxide nanotube and a hydrogen peroxide solution to obtain 2-chloro-6H-dibenzothiazine dioxide; the preparation method comprises the following steps: reacting 2-chloro-6H-dibenzothiazine dioxide, zinc powder and glacial acetic acid to obtain an intermediate; and mixing the intermediate, p-toluenesulfonic acid and a solvent, and carrying out microwave-assisted hydrolysis to obtain 4 '-chloro-2-aminobiphenyl. The method has the effects of improving the yield and purity of the product, and meanwhile, the environmental protection property and economical efficiency of the process are improved.

The present invention relates to an improvement in the detection technology of Aβ fibrils, in particular to a microenvironment-sensitive fluorescent dye for detecting Aβ fibrils and a preparation method thereof; aiming at the deficiencies of commercially available dyes for detecting Aβ fibrils in terms of poor specificity, low binding affinity, and poor signal-to-noise ratio, a novel class of D-π-A type benzothiazine-based boron fluoride dyes that are sensitive to both the polarity and viscosity of the microenvironment of Aβ fibrils is invented; the boron fluoride fluorescent dye synthesized in the present invention can change parameters such as its fluorescence wavelength and fluorescence quantum yield according to the changes in the polarity and viscosity of Aβ fibrils, and can meet the requirements for detecting Aβ fibrils with high sensitivity and high signal-to-noise ratio. In addition, the boron fluoride fluorescent dye synthesized in the present invention has a good linear configuration and is easy to enter the hydrophobic cavity of Aβ fibrils, thereby improving the binding affinity and selectivity of the dye to Aβ fibrils.

The present invention belongs to the technical field of heterocyclic compounds, and specifically relates to a 1,2-benzothiazine Schiff base derivative and a preparation method thereof. 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid methyl ester-1,1-dioxide and hydrazine hydrate are refluxed to obtain 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid hydrazide-1,1-dioxide; 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid hydrazide-1,1-dioxide is reacted with potassium ferrocyanide to obtain 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid hydrazide-1,1-dioxide; 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid hydrazide-1,1-dioxide is refluxed with o-anisidine to obtain 1,2-benzothiazine Schiff base derivative. The present invention has good anti-tumor activity.

This invention relates to the field of fine chemical technology and discloses a method for preparing N-methyl-2,3-dihydrobenzothiazin-4-one. Specifically, the method involves using 2-mercapto-N-methylbenzamide and 1-(chloromethyl)-1,4-diazabicyclo[2.2.2]octane-1-ammonium chloride (DABCO•DCM) as raw materials, with hydroiodic acid (HI) as an important additive. A one-step reaction is carried out in acetonitrile at 100-120°C. After purification, the target product, N-methyl-2,3-dihydrobenzothiazin-4-one, is obtained. This method is simple to operate, has a high yield, and does not require the use of formaldehyde, a carcinogen, as a reactant, making it potentially applicable.

This invention provides a benzothiadiazine 1,1-dioxide compound, its preparation method, and its applications. The general structural formula of the benzothiadiazine 1,1-dioxide compound is shown in Formula (I), or its isomers, or pharmaceutically acceptable salts, esters, or prodrugs thereof. The benzothiadiazine 1,1-dioxide compound of this invention has a novel structure, can selectively inhibit HDAC6 enzyme, has a strong protective effect on nerve cells, low toxicity, and low potential cardiotoxicity, and is expected to be used as a neuroprotective agent for the treatment of neurodegenerative diseases.

The invention relates to an aqueous biocide composition, containing the following components: (a) 9 wt. % to 20 wt. % 1,2-benzisothiazolin-3-one, (b) a dissolved alkalizing agent, containing 0.95 to 1.05 mol sodium and potassium hydroxide, each based on one mol of the 1,2-benzisothiazolin-3-one present as component (a), and (c) more than 60 wt. % water. The biocide composition is characterized in that the composition: (i) has a pH value in the range of pH 9.5 to pH 11.9, and (ii) the molar fraction of sodium ions, based on the sodium and potassium ions present in the composition, is in the range of 15 to 45 mol %. The invention furthermore relates to the use of these biocide compositions for preserving water-based products of all kinds, such as cleaning and household products, plastic dispersions, paints, plasters, adhesives, sealing compounds, paper coating compounds, textile softening and sizing agents, detergent base materials, surfactants, polishing agents, spinning baths, cooling lubricants, leather treatment agents, and silicone and bitumen emulsions.

The present invention relates to dihydroquinazoline, dihydrobenzothiazine and dihydrobenzoxazine derivatives for use in the prevention or treatment of neurological, psychiatric, sleep disorders and diseases, advantageously in which central orexin neurotransmission is impaired or in which central and peripheral orexin receptors are involved. The invention also relates to pharmaceutical compositions comprising these compounds, their use for the prevention and / or treatment of nervous system disorders and diseases. The invention also relates to dihydroquinazoline, dihydrobenzothiazine and dihydrobenzoxazine derivatives, and to the use of these compounds as medicaments.

The application belongs to the technical field of medicine, and particularly relates to an arylalkyl azole derivative, a preparation method and application thereof. The arylalkyl azole derivative is obtained by directly connecting 4H-1,2,4-triazole-4-yl to benz[d][1,3]thiazine as aryl through a chemical bond and introducing an alkoxy group at the C6 position of the aryl. The compound of the application has a novel structure, and as a GABA_A receptor agonist, exhibits excellent anticonvulsant activity in two kinds of epilepsy models of maximum electric shock and subcutaneous pentylenetetrazole. In particular, the compound exhibits an extremely high protection index PI>10 in the subcutaneous pentylenetetrazole model, indicating that the compound has the remarkable advantages of diverse action mechanism, wide therapeutic window and low neurotoxicity, and can be used for preparing an antiepileptic drug, and is particularly suitable for the treatment of refractory epilepsy.

The present invention is directed to dihydroquinazoline, -benzothiazine and -benzoxazine derivatives, advantageously for use in the prevention or treatment of neurological, psychiatric and sleep disorders and diseases in which central orexin neurotransmission is impaired or in which central and peripheral orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds for use in the prevention and / or treatment of neurological disorders and diseases. The present invention is also directed to dihydroquinazoline, -benzothiazine and -benzoxazine derivatives and the use of these compounds as medicaments.