49 results about "Dihydropyran" patented technology

The invention provides an engineered ketoreductase mutant, which comprises a polypeptide sequence, a gene sequence, a recombinant expression vector containing the gene, an engineering strain, a protein expression method of the engineering strain, and a reaction process for selectively synthesizing (R)-5, 7-difluorochroman-4-ol by using the engineered ketoreductase mutant.

This disclosure provides compounds of Formula ( AA ) Formula ( A ), Formula ( I ) (e.g., Formula ( I-a1 )), Formula ( II ) (e.g., Formula ( II-1 ), ( II-a ), ( II-a1 ), ( II-a2 ), or ( II-a3 )), Formula ( III ) (e.g., Formula ( III-1 )), Formula ( IV ) (e.g., Formula ( IV-a ), ( IV-a1 ), ( IV-b ), ( IV-b1 ), or ( IV-c )), or Formula ( B ) (e.g., Formula ( B-1 )), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein. In some embodiments, the KRas protein has a dysregulation (e.g., the KRas protein is mutated or amplified). These compounds are useful, for example, for treating a disease, disorder, or condition in which increased and / or sustained (e.g., excessive) KRas activation, for example, KRas activation associated with a mutant KRas protein, contributes to the pathology and / or symptoms and / or progression of the disease, disorder, or condition (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing compounds as disclosed herein, or pharmaceutically acceptable salts thereof, and methods of using and making the same.

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.

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 discloses a preparation method of 3,4-dihydropyran derivatives, and a reaction formula is as follows: the unactivated propenal and the weak polar olefin which are simple in structure and low in material cost are used as starting materials, the unactivated propenal and the weak polar olefin which are weak in reactivity can participate in [4+2] cycloaddition, and the 3,4-dihydropyran derivatives with high purity can be prepared; the preparation process is simple in operation, high in yield and excellent in diastereoselectivity, can effectively convert low-cost raw materials into high-value-added compounds, and provides an economic and efficient synthesis strategy for related industries.

Derivatives of Sabinene (1-isopropyl-4-methylenebicyclo[3.1.0]hexane, CAS No. 3387-41-5), as well as their synthesis and use in organoleptic applications, are described herein. The Sabinene derivatives include a compound having a general Formula (I), wherein --- is a single or a double bond; wherein if --- is a single bond, then Y is selected from the group consisting of CH2R1, CH=C(R2)R3, and (CH2)xCHR3R4; and OR5; wherein if --- is a double bond, then Y is O, N-OMe, or N-OEt; R is selected from the group consisting of H, C(O)-R6, and CH(R6)-OR5; R1 is selected from the group consisting of 1,3-dioxepan, 5-methyl-1,3-dioxolan-4-one, (CH=CH)x(CH2)nOH, (CH=CH)x(CH2)nCHO, CH(CH3)CO2Et, and CH(CH3)OH; R2 = H or Me; R3 is selected from the group consisting of CHO, CO2Et, (CH2)nOH, (CH2)nCHO, (CH2)nCN, and (CH2)nCO2Bu; and R4 is CHO or CH2OH; or R3 and R4 in combination form a dihydropyran, a tetrahydropyran, a tetrahydropyranol, a tetrahydropyranone, a dimethylcyclohexenone, or a dimethylcyclohexenol; R5 is selected from the group consisting of CH(CH3), CH(CH2CH3), C(CH3)CH3, and C(CH3)CH2CH3; R6 is selected from the group consisting of OMe and Me; x is an integer selected from 0 or 1; and n is an integer selected from 2 to 7; with the proviso that when --- is a double bond and Y is O, then R and R6 are not H.

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 present disclosure provides compounds of formula (A) (e.g., formula (I) (e.g., formula (I-a1), (I-a2), (I-a3), (I-a4), (I-a5), (I-b1), (I-b2), (I-b3), (I-b4), (I-b5), or (I-c1)), formula (II) (e.g., formula (II-a), (II-b), (II-a1), (II-b1), (II-a2), or (II-b2)), formula (III) (e.g., formula (III-1) or (III-2)), which inhibit KRas protein. Provided are compounds of Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), or (IV-b2)), or Formula (V) (e.g., Formula (Va) or (Vb), (V-a1), (Vc), (Vd), (V-b1), (V-a2), or (V-b2)), or Formula (VI) (e.g., Formula (VI-a), (VI-b), (VI-c), (VI-d), or (VI-e)), or a pharmaceutically acceptable salt thereof. These compounds are useful, for example, for treating diseases, disorders, or conditions in which increased and / or sustained KRas activation (e.g., KRas activation associated with a mutant KRas protein) contributes to the pathology and / or symptoms and / or progression of the disease, disorder, or condition. The present disclosure also provides compositions containing the compounds provided herein or pharmaceutically acceptable salts thereof. TIFF2025541682000773.tif91128

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 present disclosure provides suspendable ophthalmic solutions with excellent redispersibility. The present disclosure provides an aqueous suspension agent comprising (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, a cellulosic polymer, and a nonionic surfactant.

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.

This disclosure provides compounds of Formula ( AA ), Formula ( A ) (e.g., Formula ( I-a1 )), or Formula ( B ), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein. In some embodiments, the KRas protein has a dysregulation (e.g., the KRas protein is mutated or amplified). These compounds are useful, for example, for treating a disease, disorder, or condition in which increased and / or sustained (e.g., excessive) KRas activation, for example, KRas activation associated with a mutant KRas protein, contributes to the pathology and / or symptoms and / or progression of the disease, disorder, or condition (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing compounds of Formula ( AA ), Formula ( A ) (e.g., Formula ( I-a1 )), or Formula ( B ), or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

The present disclosure provides Formula (A) (e.g., Formula (I) (e.g., Formula (I-a1), (I-a2), (I-a3), (I-a4), (I-a5), (I-b1), (I-b2), (I-b3), (I-b4), (I-b5), or (I-c1)), Formula (II) (e.g., Formula (II-a), (II-b), (II-a1), (II-2)), Formula (III) (e.g., Formula (III-1) or (II-2)), Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), or Formula These compounds are useful, for example, in the treatment of a disease, disorder or condition in which increased and / or sustained KRas activation (e.g., KRas activation associated with a mutant KRas protein) contributes to the pathology and / or symptom and / or progression of the disease, disorder or condition. The present disclosure also provides compositions containing these compounds provided herein or pharmaceutically acceptable salts thereof.

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.

To provide an efficient method for producing (2R)-1-(morpholin-4-yl)-2-[(oxan-2-yl)oxy]propan-1-one.SOLUTION: In one aspect, there is provided a method for producing (2R)-1-(morpholin-4-yl)-2-[(oxan-2-yl)oxy]propan-1-one. This production method comprises contacting (2R)-2-hydroxy-1-(morpholin-4-yl)propan-1-one and 3,4-dihydro-2H-pyran in the presence of pyridinium paratoluenesulfonate at a temperature of 40°C or higher.SELECTED DRAWING: None

The invention relates to the technical field of chemical synthesis, and discloses a preparation method of 2-[2-(tetrahydropyranyl) oxy] methyl propionate. The preparation method of the 2-[2-(tetrahydropyranyl) oxy] methyl propionate comprises the following steps: taking methyl lactate and 3, 4-dihydro-2H-pyran as reaction raw materials, reacting under the catalysis of an IL1 / MCM-41 catalyst and a solvent-free condition, and after the reaction is finished, separating the catalyst to obtain a finished product of the 2-[2-(tetrahydropyranyl) oxy] methyl propionate. The IL1 / MCM-41 catalyst is a heterogeneous catalyst formed by loading a disulfonic functionalized ionic liquid IL1 on an MCM-41 mesoporous molecular sieve. The preparation method disclosed by the invention is mild in reaction condition, simple and convenient to operate, high in conversion rate and selectivity, and capable of meeting green chemical requirements, and has a remarkable industrial application prospect, and the catalyst can be recycled through simple filtration and can be repeatedly used for multiple times.

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.

In the production of crops in agriculture, horticulture and the like, the damage caused by insect pests and the like is still large, and the development of a novel pest control agent is desired in view of the factors such as the development of insect pests that are resistant to existing drugs, and the like. The present invention provides compounds represented by the formula (1) wherein X and Y are oxygen atoms or sulfur atoms, Z is a hydroxyl group or the like, R1 is a hydrogen atom or the like, R2, R3 and R4 are hydrogen atoms and the like, and R5 and Q are substituted phenyl groups and the like, or salts thereof, pest control agents containing the compounds as active ingredients, and methods for use thereof.

The application provides a whitening composition, a preparation method and application thereof, and belongs to the technical field of cosmetics. In the whitening composition provided by the application, lauroyl sarcosine isopropyl ester, diisopropyl sebacate, PPG-14 polyglyceryl-2 ether, bis-diethoxydiglycol cyclohexane 1,4-dicarboxylic acid ester and poly C10-30 alkylol propenoate are used as oil phases to wrap whitening components (magnolia alcohol, pterostilbene, ferulic acid and dimethyl methoxy benzodihydro pyranol) to form oil capsule beads, and then the oil capsule beads are dispersed in a polyol and carbomer matrix, the composition of the oil phase and the whitening components is controlled, and the whitening effect and transdermal absorption effect of the whitening composition are improved.

The invention discloses a phosphorescent and photochromic doped luminescent material which comprises the following components in parts by weight: 1-7 parts of a phosphorescent guest compound; 1 to 7 parts of a photochromic guest compound; and 200 to 4000 parts of a host polymer. According to the doped luminescent material prepared by the invention, the phosphorescent guest compound and the photochromic guest compound are matched and doped in the host polymer, so that the photochromic and phosphorescent dual effects are realized. In particular, 11, 12-indoline [2, 3-a] carbazole or 9H-dibenzo [a, c] carbazole or halo-benzene or pyrene is used as a phosphorescent guest compound, and spiro [1, 3, 3-trimethylindole-(6 '-nitrobenzo dihydropyran)] or 2, 2'-diphenyl-3, 3 '-bibenzofuran or Arbeer-clero670 is used as a photochromic guest compound. And the photochromic and phosphorescent dual effects can be achieved. Therefore, the bottleneck that phosphorescent properties and photochromic properties are difficult to coexist in the prior art is broken through.