26 results about "Dihydropyran" patented technology

The invention discloses a fesoterodine intermediate preparation method, and belongs to the technical field of chemical medicine raw material medicine synthesis, 6-(hydroxymethyl)-4-phenylchroman-2-ol and diisopropylamine are used as starting materials to prepare a fesoterodine intermediate, an inert conversion reagent is used, and the reaction temperature is controlled to be 30-60 DEG C, so that the fesoterodine intermediate is obtained. On the other hand, the excessive diisopropylamine reacts with an inert conversion reagent, the excessive diisopropylamine is converted into an excessive state which does not react with the product, and the excessive diisopropylamine is prevented from reacting with the product to generate a large amount of various impurities; a reducing agent and an inert conversion reagent are introduced to be combined, so that the problem of impurity generation caused by palladium catalytic hydrogenation reduction is avoided.

Provided herein are compounds of Formula (II) (e.g., Formula (II-a), (II-b), (II-a1), (II-b1), (II-a2), (II-b2), (II-3), (II-a3), (II-4), (II-a4), (II-5), (II-a5), (II-6), (II-a6), (II-7), (II-a7), (II-7), or (II-a8)), Formula (III) (e.g., Formula (III-1), (III-2), (III-3), (III-4), (III-5), (III-6), (III-7), or (III-8)), Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), (IV-b2), (IV-a3), (IV-b3), (IV-a4), (IV-b4), (IV-a5), (IV-b5), (IV-a6), (IV-b6), (IV-a7), (IV-b7), (IV-a8), or (IV-b8)), Formula (V) (e.g., Formula (V-a) or (V-b), (V-a1), (V-c), (V-d), (V-b1), (V-a2), (V-b2), (V-a3), or (V-b3)), Formula (VI) (e.g., Formula (VI-a), (VI-b), (VI-c), (VI-d), or (VI-e))), or Formula (A) (e.g., Formula (I-a1)), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

The invention discloses a preparation method of a cresol trozole trisiloxane intermediate, and belongs to the technical field of fine chemical engineering. The preparation method comprises the following steps: by taking 2, 6-dibromo-4-methylphenol as a raw material, reacting with 3, 4-dihydropyran under the action of p-toluenesulfonic acid, so as to generate an intermediate 2-(2, 6-dibromo-4-methylphenoxy) pyran; reacting with sodium methoxide under the action of a catalyst to generate an intermediate 2-(2-bromo-4-methyl-6-methoxyphenoxy) pyran; then generating a Grignard reagent, carrying out coupling reaction on the Grignard reagent and 3-bromine-2-methallyl, finally reacting with benzotriazole lithium salt, and carrying out acidolysis deprotection to obtain the cresol trozole trisiloxane intermediate. The raw materials are available in the market, the overall yield is high, and a route reference is provided for synthesis of the compounds.

The application relates to a catalyst for preparing 3,4-dihydro-2H-pyran, a preparation method of the catalyst and a method for preparing 3,4-dihydro-2H-pyran by using the catalyst. The catalyst comprises a carrier, an active component and a promoter component, and is prepared by immersing the carrier in an active component precursor aqueous solution, stirring and uniformly standing, and then drying; calcining in an air atmosphere; reducing in a hydrogen atmosphere; immersing in a promoter component precursor aqueous solution, stirring and uniformly standing, and then drying; calcining in an air atmosphere; and reducing in a hydrogen atmosphere. The catalyst according to the application is applied to a process for preparing 3,4-dihydro-2H-pyran by taking tetrahydrofurfuryl alcohol as a raw material, the generation of a tetrahydropyran byproduct is reduced, the selectivity of 3,4-dihydro-2H-pyran is improved, and the difficulty of separation is reduced. The method for preparing 3,4-dihydro-2H-pyran provided by the application has the advantages of easy raw material, a more green route, simple process, high efficiency and continuous production.

The invention provides a method for catalytically synthesizing 7-amino-3-oxabicyclo [3.3. 1] nonyl-6-ene-1-ol by using rare earth, which comprises the following steps of: adding a catalyst and a catalyst, according to the preparation method, rare earth trifluoromethanesulfonate is taken as a catalyst, 6-alkoxy-2, 6-dihydropyran-3-ketone and enamine compounds are taken as raw materials, and the 7-amino-3-oxabicyclo [3.3. 1] nonyl-6-ene-1-ol is prepared by catalyzing (3 + 3) cyclization reaction. The synthesis method provided by the invention is simple in reaction raw material synthesis, low in rare earth salt price, easy in experimental operation and suitable for large-scale preparation. The obtained compound can be applied to the fields of organic synthesis, drug synthesis, organic materials and the like.

The invention provides a method for catalytically synthesizing 7-oxa-2-azabicyclo [3.3. 1] nonyl-3-ene-1-ol by using rare earth, which comprises the following steps of: adding a catalyst and a catalyst, according to the preparation method of the 7-oxa-2-azabicyclo [3.3. 1] nonyl-3-ene-1-ol, rare earth trifluoromethanesulfonate is taken as a catalyst, 6-alkoxy-2, 6-dihydropyran-3-ketone and enamine compounds are taken as raw materials, and the preparation of the 7-oxa-2-azabicyclo [3.3. 1] nonyl-3-ene-1-ol is realized. The method is simple in reaction raw material synthesis, simple in experimental operation and suitable for large-scale preparation. The obtained compound can be applied to the fields of organic synthesis, drug synthesis and the like.

This disclosure relates to a hair care composition comprising a compound that can covalently bond to hair and an excipient suitable for administration to hair, wherein the compound that can covalently bond to hair is a compound of formula (I), or its tautomers and / or pharmaceutically acceptable salts, where (I), R 1 L1 represents a protecting group that can be hydrolyzed under physiological conditions after application of hydrogen or a hair care composition to the hair, L1, L2 and L3 independently represent a linker group or are absent, and A1, A2 and A3 independently represent a)C1~C 30 Partial, H, hydroxyl, amino, or halogen, or b) C1-C 60 Represents a part or polymer part, and at least one of A1, A2 and A3 is C1-C of group b). 60 It is a part or polymer part, and C1-C of group b) 60 The present invention relates to a hair care composition in which the polymer portion is configured to act as b1) a humectant, a hair beautifying coating, or a primer for adhering dye to hair, and / or b2) a humectant, a hair beautifying coating, or a fragrance for cleavage from the 3,4-dihydro-2H-pyran portion, and L1-A1 and L2-A2 do not represent portions containing an unsaturated CC bond or CN bond at the alpha position to the carbon atoms marked "a" and "b", respectively. [Formula 1] JPEG2026520679000070.jpg29128

The application discloses a preparation method of a medical intermediate (R)-7-ethyl camptothecin, and relates to the field of chemical medicine synthesis. The application comprises the following contents: (R)-4-ethyl-4-hydroxy-7,8-dihydro-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione (formula A) and 1-(2-aminophenyl)propan-1-one (formula B) are used as main raw materials, a target compound (R)-7-ethyl camptothecin is obtained through reaction in an organic solvent under the action of a catalyst. The application provides a novel preparation method of the medical intermediate (R)-7-ethyl camptothecin, and the preparation method is simple, stable, high in yield, and suitable for industrial production.

The disclosure provides compounds of Formula (I)or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, CS, R2, and R3 are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

The application relates to a method for synthesizing dihydropyrrolo[2,3-c]pyrazole analogs. Specifically, under the catalysis of a transition metal and a bidentate ligand, dihydropyrrolo[2,3-c]pyrazole analogs can be obtained in high selectivity by using the bidentate ligand synergy, taking pyrazolinone as raw material and reacting with 1,3-alkyne under the action of triethylenediamine. The application uses cheap and commercially available 1,3-alkyne and easily obtained pyrazolinone, and a series of heterocyclic compounds with potential medicinal value are obtained in high selectivity under simple and mild conditions.

Provided herein are compounds of Formula (IV-b), or pharmaceutically acceptable salts thereof, which inhibit KRas proteins (e.g., modulate aberrant KRas proteins (e.g., mutated or amplified KRas proteins)). The disclosure also provides compositions containing a compound as provided herein, or a pharmaceutically acceptable salt thereof, as well as methods of using and preparing these compositions. Formula (IV-b).

The invention provides a detection method for lure components of a cigarette beetle trap and application of the detection method, and the detection method comprises the following steps: (1) mixing a sample to be detected with an internal standard substance and a solvent for ultrasonic treatment, and then centrifuging to obtain a liquid to be detected; and (2) carrying out gas chromatography-mass spectrometry combined detection on the to-be-detected liquid to obtain the components of the lure of the cigarette beetle trap and the content of the components. The method provided by the invention not only realizes simultaneous separation and determination of antioxidant and killing agent components in the lure of the cigarette beetle trap, but also realizes separation and determination of sex pheromones 4, 6-dimethyl-7-hydroxy-3-nonanone and 2, 6S-diethyl-3, 5S-dimethyl-2, 3-dihydropyran of cigarette beetles, sex pheromones 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z, 9Z The method provided by the invention can be used for simultaneously determining the 4, 6-dimethyl-7-hydroxy-3-nonanone isomeride, especially simultaneously separating the 4, 6-dimethyl-7-hydroxy-3-nonanone isomeride, and is high in chromatographic separation degree, accurate in qualitative analysis and good in quantitative repeatability.

The present disclosure provides a suspension-type ophthalmic solution having excellent re-dispersibility. More specifically, the present disclosure provides a water-based suspension preparation containing a first component and a second component, in which the first component is (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl) acetamide or a pharmaceutically acceptable salt or solvate thereof, and the second component comprises at least one component selected from the group consisting of diquafosol, ciclosporin, hyaluronic acid, loteprednol etabonate, bromfenac, fluorometholone and pharmaceutically acceptable salts or solvates thereof.

The present disclosure relates to a composition for preventing, alleviating or treating an eye disease, which contains (7S)-(+)-cyclopentylcarbarmic acid, 8,8-dimethyl-2-oxo-6,7-dihydro-2H,8H-pyrano[3,2-g]chromen-7-yl-ester as an active ingredient. The (7S)-(+)-cyclopentylcarbarmic acid, 8,8-dimethyl-2-oxo-6,7-dihydro-2H,8H-pyrano[3,2-g]chromen-7-yl-ester of the present disclosure exhibits the effect of remarkably reducing intraocular vascular leakage and, as such, can be advantageously used in a composition for preventing, alleviating or treating an eye disease.

The invention relates to the technical field of fine chemical engineering, in particular to a method for efficiently catalyzing the hydration efficiency of 2, 3-dihydropyran and application. The method comprises the following steps: by taking 2, 3-dihydropyran and water as raw materials and an iodine elementary substance as a catalyst, adding the 2, 3-dihydropyran, the water and the catalyst into a reactor, and producing one or more than two of 2-hydroxytetrahydropyran and derivatives thereof under the reaction conditions that the reaction temperature is 30-120 DEG C and the reaction pressure is 0-8MPa; wherein the molar ratio of the 2, 3-dihydropyran to the water is (1: 1)-(1: 10), and the dosage of the catalyst iodine elementary substance is 0.05%-1% of the mass of the dihydropyran. The addition reaction activity is obviously improved, the hydration reaction efficiency is obviously accelerated, the yield of a unit reaction device is improved, and the method has a good industrial application prospect.

A process prepares novel crystalline forms of (S)-7-oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide. The crystalline forms find application in medicaments and pharmaceutical preparations.

The application provides a pyrrolidinone and dihydropyrone compound, a preparation method and application, and belongs to the technical field of organic synthesis. Specifically, under the catalysis of a Lewis base, a pyrrolidinone and dihydropyrone compound is synthesized from a beta-oxoacrylamide and an alpha-pyrone derivative by a one-step method. The pyrrolidinone and dihydropyrone compound is synthesized by adopting the simple and easily obtained beta-oxoacrylamide and alpha-pyrone derivative as starting raw materials, and by the [3+2]-cycloaddition reaction under the catalysis of a Lewis base. The method has the advantages of simple operation, mild reaction condition, economic and easily obtained reagents and raw materials, high yield of the target product, and wide substrate application range. The method is applied to the preparation of an antitumor drug and has a good application prospect.

This invention provides a ketone reductase mutant and its application in the synthesis of a key chiral intermediate for ticoraxene. The mutant contains amino acid sequences such as SEQ ID NO: 4, 6, 8, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, or 42. This ketone reductase mutant exhibits higher carbonyl catalytic activity and chiral selectivity than the wild type, and is used in the preparation of the key intermediate R-5,7-difluorobenzodihydropyran-4-ol for ticoraxene.

The present disclosure provides a compound of formula (I-c) or a pharmaceutically acceptable salt thereof that inhibits the KRas protein. In some embodiments, the KRas protein has a modulation disorder (e.g., the KRas protein is mutated or amplified). These compounds are useful, for example, in the treatment of a disease, disorder or condition in which increased and / or sustained (e.g., excessive) KRas activation, such as KRas activation associated with a mutant KRas protein, contributes to the pathology and / or symptom and / or progression of a disease, disorder or condition (e.g., cancer) in a subject (e.g., a human). The disclosure also provides compositions containing a compound of formula (A) (e.g., formula (I) (e.g., formula (I-a), (I-b), (I-c), (I-d), (I-c2), (I-c3), (I-c4), (I-d), or (I-e)) or formula (B), or a pharmaceutically acceptable salt thereof, as well as methods of use and preparation thereof. And (I-c).

The present invention is entitled "A Continuous Flow Preparation Method for Tegoragen Intermediates", belonging to the field of chemical synthesis technology. The technical problem to be solved is that the existing preparation methods have safety risks, long reaction time and low yield. The key points of the technical solution are as follows: The continuous flow preparation method of the present invention is as follows: (1) 3,5-difluorophenol and 3-chloropropanol are dissolved in organic solvents to form solutions, and then reacted with organic amines in a microreactor. After the reaction is completed, the material is discharged and the organic layer 1 is separated; (2) 2,2,6,6-tetramethylpiperidine oxide is added to the organic layer 1, and then reacted with sodium hypochlorite solution and sodium chlorite solution in a microreactor for oxidation reaction. After the reaction is completed, the material is discharged and the organic layer 2 is separated; (3) The organic layer 2 is then reacted with concentrated sulfuric acid in a microreactor. After the reaction is completed, the material is washed with water and the organic layer 3 is separated. After concentration and recrystallization, the tegoragen intermediate 5,7-difluorobenzodihydropyran-4-one is obtained.

The present disclosure relates to a hair care composition comprising a compound capable of covalently binding to hair and an excipient suitable for application to hair wherein the compound capable of covalently binding to hair is a compound of formula (I) or a tautomer and / or a pharmaceutically acceptable salt thereof, (I); wherein R1 represents hydrogen or a protecting group that is hydrolysable under physiological conditions upon application of the hair care composition to hair; wherein L1, L2 and L3, independently of each other, represent a linking group or are absent, and wherein A1, A2 and A3, independently of each other, represent: a) a C1-C30 moiety, H, hydroxyl, amino or halogen, or b) a C1-C60 moiety or a polymeric moiety; wherein at least one of A1, A2 and A3 is a C1-C60 moiety or a polymeric moiety of group b); wherein the C1-C60 portion or polymeric portion of group b): b1) is configured to act as a humectant, a cosmetic hair coating or a priming cream for attaching a dye to the hair; and / or b2) is configured to act as a humectant, a cosmetic hair coating or a fragrance upon cleavage from the 3, 4-dihydro-2H-pyran moiety; and wherein L1-A1 and L2-A2 do not represent a moiety comprising an unsaturated C-C or C-N bond at the alpha position of the carbon atoms marked as "a" and "b", respectively. (I).

Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds are (3-aryl-1,2,4-oxadiazol-5-yl)-3,4-dihydro-2H-pyrano[2,3-b]pyridines of the following structure:in which Ar is aryl or heteroaryl. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2 / Smad3 signaling pathway.

The present invention relates to certain benzodihydropyranol, quinone or hydroquinone compounds and their derivatives for use in the treatment of heart failure with reduced ejection fraction (HFrEF). In particular, the present invention relates to chromanol compounds selected from the group consisting of S-(6-hydroxy-2, 5, 7, 8-tetramethylchroman-2-yl) (piperazin-1-yl) methanone and S-(6-hydroxy-2, 5, 7, 8-tetramethylchroman-2-yl) (4-(2-hydroxyethyl) piperazin-1-yl) methanone, and pharmaceutically acceptable salts thereof.

The invention discloses a resolution method of a 5, 7-difluorochroman-4-alcohol racemate, which comprises the following steps: esterifying the 5, 7-difluorochroman-4-alcohol racemate to obtain a succinic acid ester racemic mixture, and then using a safe and easily available chiral alkali as a resolving agent to synthesize the 5, 7-difluorochroman-4-alcohol racemate, thereby obtaining the 5, 7-difluorochroman-4-alcohol racemate. The preparation method comprises the following steps: firstly, preparing chiral alkali salt diastereoisomers of succinic acid ester, then carrying out purification operation to obtain optically pure single chiral alkali salt diastereoisomers of succinic acid ester, and finally, respectively carrying out acid dissociation and ester hydrolysis to obtain respective single optically pure 5, 7-difluorobenzodihydropyran-4-alcohol isomers. According to the present invention, the single 5, 7-difluorochroman-4-one isomer is prepared through the asymmetric reduction of the 5, 7-difluorochroman-4-one, such that the use of the expensive catalyst and the expensive ligand is avoided, the cost is especially low, and the application prospect is wide.