94 results about "Dihydropyran" patented technology

The invention discloses a preparation method of 3, 4-difluoro-2-methoxyphenylacetic acid, and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: reacting 2, 3-difluorophenol with 3, 4-dihydropyran under the action of sulfonic acid resin to generate an intermediate 2-(2, 3-difluorophenoxy) pyran; then lithiating, reacting with tert-butyl 2-bromoacetate, and performing acidolysis to obtain a 3, 4-difluoro-2-hydroxyphenylacetic acid intermediate; and finally reacting with a methylation reagent in the presence of alkali to generate the target compound 3, 4-difluoro-2-methoxyphenylacetic acid. The preparation method has the advantages that the route is overall reasonable, the preparation method comprises three steps, and a simple and effective new route is provided for the preparation of the 3, 4-difluoro-2-methoxyphenylacetic acid.

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.

The present invention relates to the use of compound of formula (I) as an aroma chemical to impart a fresh note, citrus note, white floral note, fruity note, herbal note, rose leaf note, steamy green note, carrot route note, woody note, pencil shaving note, remains of rose oxide note or any combination of two or more of these impressions to composition and also for enhancing and / or modifying the aroma of a composition. The present invention is further directed to a composition comprising at least one compound of formula (I) and (i) at least one aroma chemical different from the compound of formula (I) or (ii) at least one non-aroma chemical carrier, or (iii) both (i) and (ii).

The invention discloses a photocatalytic synthesis method of a trifluoromethyl-containing benzodihydropyran-4-ketone compound, which comprises the following steps: reacting a 2-allyloxy benzaldehyde compound shown as a chemical structural general formula (I) with sodium trifluoromethanesulfinate in an organic solvent under the irradiation of visible light to obtain the trifluoromethyl-containing benzodihydropyran-4-ketone compound. The benzodihydropyran-4-ketone compound containing trifluoromethyl is obtained, and the structural general formula of the benzodihydropyran-4-ketone compound containing trifluoromethyl is shown in a formula (II). The synthesis method provided by the invention adopts low-cost sodium trifluoromethanesulfinate as a raw material, does not need to additionally add a transition metal catalyst, a photocatalyst, an oxidizing agent and the like, and has the characteristics of mild reaction conditions, simple synthesis and post-treatment processes, high reaction atomic efficiency, high target product yield, low preparation cost, environmental friendliness and the like; the method is suitable for large-scale industrial production application.

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 relates to the technical field of medicine preparation, discloses a synthesis method for constructing 4-substituted isocoumarin and analogues thereof through ring opening of oxetane, and synthesizes a series of isocoumarin derivatives. Comprising isocoumarin derivatives with 4-position hydroxymethyl substitution and 4-position amidomethyl substitution, and isocoumarin series compounds composed of five-membered heteroaromatic rings and dihydropyrone, and the synthesized isocoumarin series compounds have a plurality of functionalization sites, can be used as common intermediates in pharmaceutical chemistry research to rapidly provide series derivatives, and can be used for preparing the isocoumarin series compounds. Reaction raw materials and reagents used are convenient and easy to obtain and low in price, reaction conditions in the reaction process are mild, the process is simple, harsh conditions such as high temperature and high pressure are not needed, and the generated product does not contain metal ions, is convenient to separate and purify and is suitable for large-scale production in factories.

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.

A synthesis method of benzodihydropyran compound II with aziridine structure fragments comprises following steps: 1, preparing compound II-6 by using compound II-5 as reaction raw material, namely # imgabs 0 #, 2, preparing compound II-7 by reacting compound II-6 with alkali for cyclization, namely # imgabs 1 #, 3, and reacting compound II-7 with intermediate HO-Rw to obtain compound II, namely # imgabs 2 #.

The present invention relates to 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, processes for their preparation, medicaments and pharmaceutical formulations comprising these forms.

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 present invention relates to a process for the production of chromanol and 2-methyl-1,4-naphthoquinone derivatives, more specifically to a process for preparing a compound of the general formula (I) or (II) wherein the variables are as defined in the claims and the description.

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 present invention relates to 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, processes for their preparation, medicaments, and pharmaceutical compositions containing these forms.

The present invention belongs to the field of organic synthesis and specifically relates to a method for synthesizing 2'-fluoro-2'-deoxyuridine and its intermediates. The method comprises the following steps: The method prepares 2'-fluoro-2'-deoxyuridine by constructing novel intermediates, namely, compounds of formula IV, III, and II. This method avoids the use of reagents such as dihydropyran, which are strong eye and skin irritants. The method results in milder reaction conditions, lower costs, simple operation, environmental friendliness, high yield, and suitability for industrial production.

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.

Poly(cyclic vinyl ethers) (PCVEs), compositions of same, methods of making same, and uses of same. In various examples, PCVEs (e.g., homopolymers and / or copolymers) comprise repeat units comprising cyclic vinyl ether (CVE) groups in the backbone (e.g., poly(2,3-dihydrofuran) and / or poly(3,4-dihydropyran)). In various examples, PCVE homopolymers comprise molecular weights (Mn and / or Mw) of 200 kilodalton (kD) or greater. In various examples, PCVE copolymers (e.g., random or block) comprise one or more CVE group(s) and / or additional (e.g., acyclic vinyl ether (AVE) and / or styrenic) group(s)). A method of preparing PCVEs comprises polymerizing monomers comprising CVE groups (e.g., 2,3-dihydrofuran and / or 3,4-dihydropyran). In various examples, pentakis(carbonylcyclopentadienes) (PCCPs) and / or hydrogen bond donors are polymerization catalysts and / or initiators. various examples, PCVEs are biorenewable, recyclable, thermoplastic materials that exhibit desirable optical clarity, desirable barrier properties to, e.g., oxygen, carbon dioxide, and water, and find uses in food packaging, windows, 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 invention discloses a preparation method of a trifluoromethyl substituted chroman-4-one compound, and relates to the technical field of organic matter synthesis. According to the method, a Togni's reagent is used as a trifluoromethyl source, various 2-allyloxy benzaldehyde compounds are used as substrates, and a nonmetal photosensitizer is used, so that synthesis of various trifluoromethyl substituted chroman-4-ones and derivatives thereof is realized. By optimizing the synergistic effect of the photosensitizer and the light source, substrate limitation is broken through, the reaction stability is improved, and the problems that in the prior art, substrate applicability is limited, light source dependency is high, and the substrate yield is unstable are solved.

The invention relates to a template molecule, a molecularly imprinted polymer and application of the molecularly imprinted polymer in separation of naringin, and belongs to the technical field of plant component refining. According to the molecularly imprinted polymer disclosed by the invention, (S)-2-(4-hydroxymethyl phenyl)-7-(((2S, 3R, 4S, 5S, 6R)-3, 4, 5-trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yl) oxy) benzodihydropyran-4-one is used as a template molecule, and the template molecule and a target product naringin can form multiple acting sites through non-covalent bonds such as hydrogen bonds and hydrophobic interaction, so that the target product naringin can be used for preparing the target product naringin. Therefore, specific binding is carried out, namely, high selectivity to naringin is achieved. The virtual template molecule is low in cost and can be used for large-scale preparation of molecularly imprinted polymers, and the extraction cost of naringin is remarkably reduced.

The invention discloses a total synthesis method and application of furanose ring pyrrole spiroketal alkaloid, and belongs to the technical field of chemical synthesis and biological medicine. According to the method, D-glucose is used as a raw material and reacts with dibenzylamine, 1-dibenzylamino-1-deoxy-D fructose is prepared through an Amadori rearrangement reaction, 1-amino-1-deoxy-D fructose is prepared through direct hydrogenation debenzylation, or 2-hydroxyl of 1-dibenzylamino-1-deoxy-D fructose is protected by adding methyl and then debenzylation protection is carried out, and 1-amino-1-deoxy-D fructose is obtained. The preparation method comprises the following steps: preparing 1-amino-1-deoxy-2-methoxyl-D-fructose; and respectively carrying out Maillard condensation reaction on the two obtained amino sugars and dihydropyrone, and then completing spiro reaction under an acidic condition to obtain acorine B and pinosine C. The acorine B and pinosine C synthesized by the invention can obviously reduce the weight of an aged mouse, reduce the fat index, reduce lipid droplets in the liver and fat in thymus, reduce the number of aged cells and improve the proportion of T cells in immune cells, and have the potentials of reducing fat and resisting immune aging.

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 invention discloses a method for enhancing the hydration efficiency of 2, 3-dihydropyran. According to the present invention, 2, 3-dihydropyran and water are adopted as raw materials, alcohol chemicals are adopted as additives, and reaction is performed at a temperature of 80-160 DEG C and a pressure of 0.5-8 MPa in the presence or absence of an acid catalyst to produce the 2-hydroxytetrahydropyran and the derivative thereof. According to the method, the contact interface between the 2, 3-dihydropyran and the water raw material is promoted by using the additive, the addition reaction activity is improved, the hydration reaction efficiency is enhanced, the yield of a unit reaction device is improved, and the method has a good industrial application prospect.

A method for detecting Ag based on phenothiazine + and ClO ‑ The fluorescent probe Tz3 and its preparation method and application relate to the technical field of fluorescent probes. Sodium carbonate is first added to dichloromethane, and then a mixture of 11-ethyl-2-oxo-2,11-dihydropyrano[2,3-b]phenothiazine-3-carbonyl bromide and dimethylpyridinamine is added, followed by stirring at room temperature for reaction. The reaction is completed by TLC detection to obtain the fluorescent probe Tz3. The present invention can distinguish Ag + and Hg 2+ , with good selectivity, anti-interference and sensitivity.

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.