11 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.

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.]

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.

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 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 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.

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