21 results about "Sulfinamide" patented technology

This invention discloses an analytical method for benzothiazole contaminants, comprising the following steps: detection by high performance liquid chromatography (HPLC), with the following chromatographic conditions: a phenylhexyl column as the stationary phase, mobile phase A being water, mobile phase B being acetonitrile, and gradient elution; wherein the benzothiazole contaminants are at least one of 2-aminobenzothiazole, 2-hydroxybenzothiazole, benzothiazole, 2-methylbenzothiazole, 2-mercaptobenzothiazole, 2,5-dimethylbenzothiazole, 2-cyanobenzothiazole, ethyl 2-carboxylate benzothiazole, 2-chlorobenzothiazole, 2-bromobenzothiazole, 2-methylthiobenzothiazole, phenylthiocyanate, N-tert-butyl-2-benzothiazole sulfenamide, 2-(2-hydroxyphenyl)-benzothiazole, N-cyclohexyl-2-benzothiazole sulfinamide, dibenzothiazole disulfide, and N,N-dicyclohexyl-2-benzothiazole sulfonamide.

A process for manufacturing a rubber composition which comprises more than 50 phr of a diene elastomer rich in ethylene units, a reinforcing filler comprising a carbon black and a vulcanization system comprising sulfur, a sulfenamide as primary accelerator and a thiuram polysulfide or a mixture of a thiuram polysulfide and a guanidine as secondary accelerator is provided. The process comprises mixing the highly saturated diene elastomer, the reinforcing filler and the secondary accelerator by kneading at a temperature above 110° C., in the absence of the sulfur and the primary accelerator, and incorporating the sulfur and the primary accelerator into the rubber composition by kneading at a temperature below 110° C. The process makes it possible to reduce the hysteresis of the vulcanized rubber compositions.

The invention discloses a preparation method of (R)-(+)-tert-butyl sulfinamide. The preparation method comprises the following steps: 1, chlorinating a compound I to obtain a compound II; 2, substituting the compound II to obtain a compound III; 3, carrying out chiral oxidation on the compound III to obtain a compound IV; and 4, carrying out N-deprotection on the compound IV to obtain a compound V. According to the method, tert-butyl mercaptan is taken as a raw material, and the target product (R)-(+)-tert-butyl sulfinamide is obtained through four-step reaction of chlorination, substitution, chiral oxidation and deprotection. The safety risk of materials used in the reaction is low, compared with a traditional route, liquid ammonia is not needed to serve as a solvent for cryogenic reaction, the equipment requirement is low, operation is easy, the three-waste amount is small, the yield is high, the product quality is high, and the method is suitable for industrial production.

The weldable ultralow-temperature conductive silver paste comprises the following components: silver powder, an organic solution, an adhesive, an auxiliary agent, a curing agent and a filler, the silver powder is formed by mixing flaky micron silver powder and nano spherical silver powder; the organic solution is one of ethanol, isopropanol and dimethyl sulfinamide; the adhesive is macromolecular resin, and the macromolecular resin is formed by mixing epoxy resin and polyester resin; the auxiliary agent is a surfactant, and the main component of the auxiliary agent is polyvinyl alcohol; the curing agent is one of phthalic ester, a silane coupling agent, modified dicyandiamide and amino resin; according to the invention, through cooperative use of high-molecular resins with different molecular weights and solvents with different dissolving capacities, the adhesive force between the slurry and a base material is greatly improved, the viscosity of the slurry is adjustable, and the leakage property and the surface flatness of a coating film during printing are improved by adding the leveling agent.

The purpose of the present invention is to provide a compound that has an excellent effect of inducing BRD4 protein degradation and is useful as a cancer therapeutic agent, or a pharmaceutically acceptable salt thereof. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof. [In the formula, each symbol is as defined in the description.]

The application relates to the technical field of lithium ion batteries, in particular to an electrolyte and a lithium ion battery comprising the electrolyte. The electrolyte comprises a lithium salt, an organic solvent and an additive; the additive comprises an additive A and an additive B; the additive A is a sulfonamide compound or a sulfinamide compound; and the additive B is a thiophene silicon cyanide compound. Through the synergistic effect of the sulfonamide compound and / or the sulfinamide compound and the thiophene silicon cyanide compound, the high-pressure resistance of the battery can be effectively improved, and the low-temperature performance and the cycle performance of the battery can be considered.

The application relates to the technical field of organic synthesis, and provides a synthesis method of chiral allylamine and application thereof, which takes isoegual and chiral tert-butylsulfonamide as initial raw materials, synthesizes an enamine intermediate M1, adopts a silyl ether protecting group to protect a phenolic hydroxyl group to obtain an intermediate M2, then carries out a Grignard reaction on the intermediate M2 to obtain an intermediate M3, then removes a sulfinyl group from the intermediate M3 to obtain an intermediate M4, and then acetylates to obtain an intermediate M5, and finally removes a silyl ether protecting group from the intermediate M5 to obtain the chiral allylamine. The synthesis method can reduce the preparation cost of the chiral allylamine, is beneficial to industrialized production, optimizes stereoselectivity, and omits a chiral resolution step, and the chiral allylamine can be used for synthesizing colchicine.

This invention discloses a novel chiral sulfinamide monophosphine ligand based on an oxanthracene skeleton, its preparation method, and its application. The preparation method includes the following steps: (1) oxanthracene is subjected to a substitution reaction with RBr in the presence of sodium hydride and a solvent to obtain intermediate 1; (2) intermediate 1 is subjected to lithium halide exchange with butyllithium in the presence of a solvent, followed by the addition of a halogen to obtain intermediate 2; (3) intermediate 2 is subjected to halogen-metal exchange with isopropylmagnesium chloride in the presence of a solvent, followed by the addition of diphenylphosphine chloride to undergo a substitution reaction to obtain intermediate 3; (4) intermediate 3 is subjected to lithium halide exchange with butyllithium in the presence of a solvent, followed by the addition of a compound to react in the presence of a Lewis acid to obtain the chiral sulfinamide monophosphine ligand. The chiral sulfinamide monophosphine ligand prepared by this invention can be used to prepare chiral α-alkyl-α-benzyltetrahydronaphthone compounds with high yield and ee value.

The invention belongs to the technical field of pharmaceutical chemicals, and particularly discloses a bicyclo [2.1. 1] hexane derivative as well as a preparation method and application thereof. The bicyclo [2.1. 1] hexane derivative is a compound as shown in a formula (I) or a formula (II), a pharmaceutically acceptable salt, a stereoisomer or an isotope label of the bicyclo [2.1. 1] hexane derivative, wherein R1 is optionally selected from C1-C6 alkyl groups, bromomethyl alkyl, benzyl alkyl, ester groups, acylamino and acyl groups; r2 is optionally selected from hydrogen, C1-C6 alkyl, benzyl alkyl, aryl, heteroaryl, alkenyl, halogen and silicon; r3 is optionally selected from hydrogen, C1-C6 alkyl, bromomethyl alkyl, benzyl alkyl, an ester group, an acylamino group, an acyl group, an amido group, a sulfenamide group, halogen and a carboxyl group; and R4 is optionally selected from C1-C6 alkyl, benzyl alkyl, aryl, heteroaryl and alkenyl. And the formula (II) can be obtained by carrying out half-pinacol intramolecular rearrangement on the formula (I). Tests prove that the compounds in the formula (I) and the formula (II) can be used for treating osteoarthritis diseases.

This invention relates to a chiral sulfinamide carboxylic acid compound, its synthesis method, and its applications. The chiral sulfinamide carboxylic acid compound has the structure of formula (1), and its main structural feature is the simultaneous presence of a carboxylic acid and a chiral sulfinamide substituent at the ortho position of a heteroaromatic ring. The substituent in the chiral sulfinamide can be aryl or alkyl, while the heteroaromatic ring can be a mono- or poly-substituted benzene ring, a mono- or poly-substituted naphthalene ring, a thiophene ring, or a furan ring and a pyridine ring. The synthesis of this chiral sulfinamide is simple, using inexpensive and readily available raw materials, with mild reaction conditions and easy operation. This chiral carboxylic acid is a novel protonic acid chiral catalyst. It is particularly suitable for transition metal-catalyzed asymmetric reactions, producing products with high yields and enantioselectivity.

The purpose of the present invention is to provide a compound that has an excellent effect of inducing BRD4 protein degradation and is useful as a cancer therapeutic agent, or a pharmaceutically acceptable salt thereof. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof. [In the formula, each symbol is as defined in the description.]

The application provides a method for efficiently synthesizing chiral sulfenamide, and the specific synthesis method is as follows: aryl / alkenyl borate is used as raw material, and nickel-catalyzed asymmetric addition reaction is used to convert sulfenamide into chiral sulfenamide. The key of the application is that a chiral anion ligand is combined with divalent nickel to generate a high-activity catalytic species which is stable in structure and excellent in catalytic performance, and a series of chiral sulfenamide compounds are constructed. The application has good substrate compatibility, aryl / heteroaryl and alkenyl borate can all react, and the enantioselectivity control is excellent. In the amplification experiment with a scale of 5mmol, the catalyst consumption can be reduced to 0.5%, and the application has potential industrial application prospect.

The invention discloses a beta-sulfinyl imide ester-based aza-sulfur chiral center asymmetric construction method, which comprises the following steps: adding a beta-sulfinyl imide ester compound, a catalyst and an alkaline compound into an organic solvent, cooling the reaction mixture to-40 DEG C, stirring for 3 minutes, then adding a halogenated alkane compound, and reacting for 3 minutes at the temperature of-40 DEG C to obtain the aza-sulfur chiral center asymmetric construction method based on beta-sulfinyl imide ester. And continuously stirring at-40 DEG C for 48 hours, and after the reaction is finished, purifying through rapid column chromatography to obtain the target product chiral thioimine. The molar ratio of the beta-sulfinyl imide ester compound to the halogenated alkane compound is 1: 1.5. The organic solvent is one of diethyl ether, ethyl acetate, tetrahydrofuran, acetonitrile and methylbenzene. According to the method disclosed by the invention, beta-sulfinyl imide ester is used as a sulfinamide anion precursor, so that the problems that the structural diversity of a target product depends on initial raw materials and the chemical space is limited in the existing method are effectively solved, the structural range of the aza-sulfur chiral center is remarkably expanded, and the preparation method is simple, mild in reaction condition and free of expensive reagents.

The application provides a chiral sulfonamide compound and a preparation method and application thereof, relates to the field of compound synthesis, and a structural general formula of the chiral sulfonamide compound is shown as formula (1). The application discloses that sodium benzenesulfinate and amine are catalyzed by a catalyst quinine or quinidine to efficiently prepare a chiral sulfonamide compound and derivatives thereof, and the chiral sulfonamide compound and derivatives thereof have excellent yield, high enantioselectivity of up to 99%, and good application potential and research value.

The invention belongs to the technical field of drug synthesis, and relates to a preparation method of chiral amino acid, which comprises the following steps: sequentially carrying out esterification reaction, reduction reaction, condensation reaction, addition reaction, acidolysis reaction, salt forming reaction, hydrolysis reaction and acylation reaction to finally prepare the chiral amino acid. According to the method, carboxylic acid serves as a starting raw material and reacts with methyl alcohol to generate methyl ester, then the methyl ester is reduced into aldehyde through diisobutylaluminum hydride, after the aldehyde and tert-butylsulfinamide are condensed under the anhydrous sodium sulfate drying condition, the aldehyde and trimethylsilyl cyanide are directly subjected to an addition reaction, and reaction liquid obtained in the fourth step is directly used for deprotection in the fifth step after being subjected to aftertreatment. After an intermediate in the fifth step is obtained, L-tartaric acid is selected as a resolving agent, a target monomer is obtained with high yield, and then the final two-step reaction is performed to obtain a target product. In conclusion, the method for preparing the chiral amino acid is simple and convenient to operate, low in cost and easy to purify, has good economical efficiency and manufacturability, and is suitable for large-scale industrial production.

The application discloses a method for preparing sulfilimine by condensation of sodium sulfinates and aromatic amines catalyzed by chiral pyridine N-oxides, and belongs to the field of organic chemistry. Sodium sulfinates and aromatic amines or alcohols are used as raw materials, and a reaction is carried out in the presence of a chiral 4-aryl pyridine N-oxide catalyst to obtain chiral sulfilimine and sulfinate, respectively. In the application, the oxygen anion in the chiral 4-aryl pyridine N-oxide catalyst acts as a nucleophilic site to participate in acyl transfer to obtain a chiral mixed anhydride intermediate, which is reacted with different nucleophilic reagents to generate chiral sulfilimine or sulfinate. The method has the advantages of good yield, high enantioselectivity, wide substrate universality and the like, and the product can also be subjected to various derivatization conversions.

The invention discloses a synthesis method of sulfonamide compounds, which comprises the following steps: mixing a sulfonamide compound containing an S-N structure, a selective fluorine reagent and water, and stirring at room temperature to realize selective oxidation of sulfonamide so as to obtain a series of sulfonamide compounds. According to the method, the synthesis of the sulfinamide compound can be efficiently realized, additional additives are not needed in the reaction, the reaction cost is reduced, the reaction is carried out in a water phase, no organic solvent is needed, and the green chemistry concept is met. The synthesis reaction operation is simple, the conditions are mild, the reaction is fast, the yield is high, the post-treatment is convenient, the amplification of the reaction can be realized, and the method has wide application prospect and practical value.

This invention discloses a catalyst-free, light-driven method for the synthesis of sulfinamide compounds, which has wide applications in organic synthesis, pesticides, pharmaceuticals, and materials science. Using alkyl alcohols and sulfinimides as reactants, this invention synthesizes a series of sulfinamide derivatives with diverse functional groups through a deoxyalkylation reaction driven solely by blue light. In this reaction, alcohols, as alkyl sources, are readily available and widely sourced chemicals. Furthermore, the use of visible light as the sole driving force eliminates the need for expensive photocatalysts, making the entire reaction process greener and more efficient. This invention provides a new approach for the efficient synthesis of sulfinamides, featuring mild reaction conditions, convenient experimental operation, good substrate compatibility, and easy scale-up, thus possessing significant application value and socio-economic benefits.

To provide a compound which is superior in an action inducing degradation of BRD4 protein and useful as a therapeutic agent for cancer, or a pharmaceutically acceptable salt thereof.SOLUTION: Provided is a compound represented by the formula (I) in the figure or a pharmaceutically acceptable salt thereof.SELECTED DRAWING: None