135 results about "Allene" patented technology

The present invention relates to 2′-allene-substituted nucleoside derivatives of the general formula (I):As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related β-D and β-L-nucleoside derivatives.

The invention relates to a blocking remover of a gas well shaft. The blocking remover comprises, by weight, 5-25% of an alcohol ether compound, 0.5-10% of a dispersant, 1-10% of a cleaning agent, and 0.5-5% of chelating agent, with the balance being a nitrogen-containing polar solvent, wherein the nitrogen-containing polar solvent is one selected from N,N dimethyl formamide, N,N dimethyl acetamide, and N-methyl pyrrolidone, the alcohol ether compound is one selected from glycol-ether, glycol-propyl ether, glycol-butyl ether, and diglycol-ether, the disperant whose micelle particle size is from 20nm to 100nm is a middle-phase microemulsion-type dispersant mixed by kerosene, water, a surfactant and a cosurfactant, the cleaning agent is one selected from allene diamine, acetonitrile and pentylamine, and the chelating agent is one selected from sodium citrate and EDTA. The blocking remover has the advantages that corrosivity is weak, that the speed of dissolving blockage is fast, that the product performance is stable in high temperatures, and that the blocking remover can reduce damages caused by water locking and fouling in areas close to gas wells, and can recover the permeability of storing layers.

The present invention relates to 2′-allene-substituted nucleoside derivatives of the general formula (I):As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related β-D and β-L-nucleoside derivatives.

The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof:which inhibit, preventing or treating abnormal cellular proliferation and / or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and / or cell proliferation. The invention also relates to methods of treating a viral infection and / or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral / anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.

The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof:which inhibit, preventing or treating abnormal cellular proliferation and / or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and / or cell proliferation. The invention also relates to methods of treating a viral infection and / or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral / anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.

The invention discloses a novel single phosphorus ligand PC-Phos of a xanthene framework. The ligand is a compound as shown in a formula (1) or an enantiomer, racemate or diastereoisomer of the compound as shown in the specification. The invention further discloses a preparation method of the ligand. A formula 2 and a formula 4 as shown in the specification serve as raw materials, and substitution reaction, addition reaction, condensation reaction and reduction reaction are performed to prepare the ligand. Alternatively, a formula 6 and the formula 4 as shown in the specification serve as raw materials, are subjected to condensation reaction and subjected to addition reaction with a formula as shown in the specification to prepare the ligand. Chiral sulfonamide 4 with two structures and different types of metallic reagents are subjected to addition reaction, and optical voidness of four full structures 1 (S, Rs), 1 (R, Rs), 1 (S, Ss) and 1 (R, Ss) of the chiral single phosphorus ligand can be obtained. The invention further discloses an application of the ligand to asymmetric cyclization reaction in catalytic allene amine molecules. The ligand has quite high reaction activity, stereo-selectivity and wide application values.

The invention relates to a high-optical-activity axial chirality allene compound and a construction method thereof. The construction method is a method for directly constructing an allene compound with axial chirality under the high stereoselectivity by performing a reaction of 2,3-allene functional group compound and a nucleophilic reagent in an organic solvent under the action of a palladium catalyst, a chiral diphosphine ligand and alkali. The method has the advantages of simplicity for operation, easiness for obtaining raw materials and a reagent and the like; the substrate universality iswide; high stereoselectivity of the product is very excellent (90 to 96%ee). The high-optical-activity allene product obtained by the method disclosed by the invention is used as an important intermediate and can be used for constructing chiral compounds, such as gamma-allenoate, gamma-allenoic acid, gamma-allenol and gamma-butyrolactone, and gamma-butyrolactone natural product (R)-traumatic lactone (98%ee) is synthesized under high enantioselectivity for the first time.

The invention discloses a method for directly constructing a high optical activity allene compound combing axial chirality and central chirality. Under effects of a palladium catalyst, a chiral diphosphine ligand and alkali, 2,3-allene function group compounds shown in a formula (1) and a nucleophilic reagent in a formula (2) are reacted in an organic solvent, and the high optical activity allene compound combing axial chirality and central chirality can be directly constructed by one step. The method has the advantages of simple operation, easy acquisition of raw material and the reagent, mild reaction condition, wide substrate universality, and good function group compatibility, and the stereoselective performance of the product is excellent (greater than 99:1 d.r., 95-greater than 99% ee). The high optical activity allene compound can be taken as an important intermediate for constructing the compounds such as monofluoro methylation allene, gamma-allene acid ester, gamma-allene acid, gamma-allenol, and gamma-butanolide containing several chiral centers.

The invention relates to a compound containing a conjugated allene amide structure and a preparation method, a medicine composition and application thereof, in particular to a compound containing a conjugated allene amide structure shown in a formula (I), and a preparation method, a medicine composition and application thereof in preparation of an EGFR (epidermal growth factor receptor) inhibitoror a medicine for preventing and / or treating EGFR-related diseases, especially cancers. (The formula (I) is shown in the description.).

The invention discloses a C3-fraction liquid phase selective hydrogenation catalyst, wherein a nano precious metal alloy active component is loaded on a carrier; the nano precious metal alloy active component comprises nanoscale alloy particles; the nano precious metal alloy active component is Pd-X, wherein the metal X is one out of Ag, Au and Cu, and the mass ratio of the alloy components Pd to X is equal to 1 to (0.2-5); the content of the nano precious metal alloy is 0.2-1.0wt% of the total mass of the carrier; the nano precious metal alloy active component is prepared by putting a bimetallic complex into a micro-emulsion system modified by a water-soluble high-molecular polymer by adopting a chemical reduction method, and loading the product onto the carrier. When being applied to a selective hydrogenation reaction of allylene and allene, the C3-fraction liquid phase selective hydrogenation catalyst has higher activity and selectivity.

The invention relates to a compound of fluoro dihydropyrrole or fluoro pyrrole and a preparation method thereof, in particular to a 4-fluorine-2, 5-dihydropyrrole compound and a 4-fluorine pyrrole compound and a novel preparation method starting from simple nitrogen-containing allene. Under the metal catalysis, N- fluorobenzenesulfonimide (NFSI) is used as oxidant and serves as a fluorine source simultaneously. The 4-fluorine-2, 5-dihydropyrrole compound is obtained in high selection mode through fluorine amination reaction of the allene. Aromatization is performed on the product to obtain the corresponding 4-fluorine pyrrole compound.

A synthesis method of alpha,alpha-difluoromethylene vinyl phosphonate having a structure represented by the formula I and having high position and high stereoselectivity is characterized by comprising the steps: with alpha,alpha-difluoromethylene-beta-allene phosphonate as a raw material, adding aryl or aromatic vinyl boric acid RB(OH)2, and under the action of a catalyst palladium acetate Pd(OAc)2 and a phosphine ligand, undergoing an aryl / vinyl hydrogenation reaction, to obtain alpha,alpha-difluoromethylene vinyl phosphonate having the E structure, wherein a substituent R is aromatic vinyl, aryl or heteroaryl. The synthesis method is simple and convenient, mild in conditions, and high in productive rate, the yield of the target fluorine-containing vinyl phosphonate can reach 71%-94%, and the E structure has high selectivity.

The invention provides a selective hydrogenation method for allylene and allene in propylene material flow. The method comprises the following steps of: introducing the propylene material flow containing 1-(methylamino)-2,3-propanediol (MAPD) and hydrogen into a hydrogenation reactor filled with a supported palladium catalyst, and performing selective hydrogenation on the MAPD in the propylene material flow at the inlet temperature of between 10 and 80 DEG C and a molar ratio of the hydrogen to the MAPD of 1-5 under the reaction pressure of 0.1-4Mpa, so that the MAPD becomes propylene and is removed, wherein the catalyst comprises a carrier, palladium and optional modifying components; and a carbon monoxide adsorption in situ infrared ray spectroscopy is used for testing the catalyst at 40DEG C, and an area ratio of a bridge absorption peak at a position of 1,930-1,990cm<-1> to a bridge absorption peak at a position of 1870-1,930cm<-1> in an infrared spectrum is less than 0.2 and preferably less than 0.15. By the method, the selective hydrogenation reaction for the allylene and allene in the propylene material flow has high selectivity, and can be stably performed for a long period.

Methods are provided for the catalytic hydroamination of compounds having an alkyne or allene functional group, in which the compound is contacted with ammonia or an amine in the presence of a catalytic amount of a gold complex under conditions sufficient for hydroamination to occur.

A method for high stereo and regioselective synthesis of medium-ring compounds of 9 to 12 rings. The product is prepared by the reaction of allenes with nucleophilic group substitution at terminal with aryl iodides or alkenyl iodides, and then mixing at 80 DEG C under the condition of taking four (triphenylphosphine) palladium chloride as catalyst, potassium carbonate as alkali, N, N-dimethyl acetamide as solvent. The invention of simple operation, high area and stereoselectivity of the reaction, easy obtained raw material and reagent, easy separation and purification products, and no need ofusing a high degree of dilution reaction conditions, which is suitable for synthesis of medium-ring compounds of 9 to 12 rings.

A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

The invention discloses a 1,1-difluoro-3-sulfonyl-2-chloro-3-butenyl phosphonate compound, a sulfonylation reaction synthetic method which adopts photoinduction and has high regioselectivity and application of the 1,1-difluoro-3-sulfonyl-2-chloro-3-butenyl phosphonate compound serving as an enzyme inhibitor in preparation of antitumor drugs. A structural formula of the compound is shown in the description, wherein substituent groups R1 and R2 are alkyl groups, or R1 and R2 are connected to form a C3-C6 naphthenic base, and R3 is selected from an alkyl group, a heterocyclic aromatic group and asubstituent or non-substituent aromatic group. Compared with the prior art, the method is a green, efficient, simple and high-regioselectivity method for synthesis of 1,1-difluoro-3-sulfonyl-2-chloro-3-butenyl phosphonate. The method is simple, mild in condition, great in substrate applicability and high in regioselectivity, the yield of target objects can reach 45-84%, and under an inductive effect of visible light, a sulfonylation reaction is carried out selectively on a 2,3-double bond of allene.

The invention discloses a method for synthesizing a 3-vinyl-4-acetenyl-2,3-dihydropyrrole derivative, and belongs to the field of chemical synthesis of allene amine cycling. The method is mainly characterized in that (1) transition metal elements are adopted for catalyzing; (2) allene is adopted as a raw material of synthesis; (3) the reaction temperature is gentle; (4) reaction is completed in one step; (5) a catalyst can be recycled and reutilized; (6) water molecules in a reaction solvent must be strictly removed, and the trace grade is achieved; (7) physical and chemical properties of a generated product cannot be changed under the environments of normal temperature and high temperature; (9) the yield of the generated product is greater than or equal to 85 weight percent; (10) a generated byproduct can be easily removed by adopting a conventional method.

The invention discloses a shock absorber top rubber formula which comprises, by weight parts, 60-80 parts of nitrile rubber, 40-60 parts of polyurethane rubber, 10-15 parts of zinc oxide, 3-10 parts of 4,4-bis-diphenylamine, 5-10 parts of poly-allene siloxane, 5-10 parts of chlorine ethyl formate, 4-8 parts of sulphur, 3-5 parts of softening oil, 5-10 parts of carbon black N330 and 1-5 parts of accelerant TMTD. Rubber prepared according to the shock absorber top rubber formula is applicable to the field of automobiles, has good oil resistance and abrasion resistance and is long in service life.

The invention relates to a method for determining contents of microscale allene and acetylene in MTO products through gas chromatography to mainly solve a problem that the determination of the content of microscale acetylene is interfered because unknown components and acetylene cannot be separated when the content of the microscale acetylene in the MTO products is analyzed through present chromatographic methods. The method comprises the following steps: injecting a sample of an analyte which is the MTO products from a chromatographic shunting introduction port (1), separating through an Al2O3PLOT capillary chromatographic column (2) deactivated by Na2SO4 or KCl, and detecting through a hydrogen flame ionization detector (3) after completely separating the allene, the acetylene and other hydrocarbon components by the chromatographic column (2). The method well solves the problem through above technical scheme, and can be applied to industrial production about the chromatographic analysis of the contents of the microscale allene and the microscale acetylene in the MTO products.

The invention discloses a synthesis method of 1,3-disubstituted allene with high optical activity, namely a method for preparing 1,3-disubstituted allene with high optical activity in one step of functionalizing terminal alkyne, aldehyde and chiral alpha, alpha-diphenyl-L-prolinol under catalysis of a bivalent copper salt. The method is simple to operate, adopts easily available raw materials and reagents, uses a substrate with wide universality, can be compatible with a plurality of functional groups, such as a plurality of glycosidic units, primary alcohol, secondary alcohol, tertiary alcohol, amides and dimethyl malonate, and does not need further protection; and the obtained axial-chirality allene is moderate to good in yield and excellent in diastereoselectivity or enantioselectivity.

The present invention provides a C3 fraction selective hydrogenation catalyst, a preparation method and applications thereof. According to the present invention, active components of the catalyst are prepared through a microemulsion method, and are loaded on a carrier, and the prepared main active component Pd of the catalyst has characteristics of small particle size, controllable particle size, and good dispersion, wherein the particle size is less than 10 nm; the catalyst preparation method has characteristics of simpleness, easy operation, and mile preparation conditions; and with application of the catalyst in selective hydrogenation reactions of propyne and allene in cracking product C3 fractions, high activity and high selectivity are provided.

The invention discloses application of an allene compound, a pharmaceutical composition containing the same and application thereof. The invention discloses application of an allene compound shown as general formula (I) in preparation of drugs for treatment of cancer. The invention also discloses a pharmaceutical composition containing the allene compound shown as general formula (I) and one or more other drugs treating cancer and application thereof in preparation of drugs treating cancer. The allene compound provided by the invention can well inhibit the growth of ovarian cancer cells, at the same time combined use of the allene compound with cis-platinum can reach stronger inhibitory effect on the tumor cells and better antitumor effect. (formula (I)).

The invention belongs to the technical field of genetic engineering, particularly relates to a method for increasing nicotine content in tobacco by utilizing camptotheca acuminate AOC (Allene Oxide Cyclase) gene transformation. In the method, a plant expression vector is constructed by using camptotheca acuminate allene oxide cyclase (AOC) genes; and the nicotine content in the tobacco is increased through over-expression of the camptotheca acuminate AOC genes in the tobacco by using a genetic engineering technology. The method comprises the process of: cloning the AOC genes from camptotheca acuminate; constructing a plant high-efficiency expression vector; introducing agrobacterium tumefaciens and performing genetic transformation on the tobacco; and measuring the nicotine content in transgenic tobacco leaves. By adopting the method, the camptotheca acuminate AOC genes can be over-expressed in the tobacco, and the nicotine content in the tobacco is increased.

The invention relates to a method for compounding a pyrroline derivative in one step by cyclizing and coupling suzuki and belongs to the field of chemical compounding of allene (1,2-propadiene) by cyclizing. The method is characterized in that (1) transition metal elements are adopted for catalyzing; (2) allene is used as a raw material for compounding; (3) the reaction is performed when the reaction temperature is low temperature or normal temperature; (4) the reaction is completed in one step; (5) the catalyst is fully recycled; (6) water is strictly removed from a reaction solvent and the trace level is achieved; (7) 2,3-pyrroline five-element ring is the main structure of the generated product; (8) the physical and chemical properties of the generated product are not changed under normal temperature and high temperature environments; (9) the yield of the generated product is more than or equal to 98 wt%; (10) the generated side products are easily removed according to a conventional method.

A photocurable composition containing at least a radical polymerizable unsaturated group-bearing compound, a metal allene compound, a squalilium dye, and N,N-dimethylaniline. The photocurable composition is polymerized and cured by generation of radicals upon receipt of low energy of visible light having long wavelengths or near infrared light.

The invention relates to a synthesis method of cyclopropyl allene derivatives. According to the method, cyclopropyl acetylene is used as starting materials for preparing metal cyclopropylacetylide and takes reaction with aldehyde for preparing cyclopropyl propargyl alcohol derivatives, hydroxyls of the cyclopropyl propargyl alcohol derivatives are protected to prepare cyclopropyl propargyl ether or cyclopropyl propargyl ester, and the cyclopropyl propargyl ether or the cyclopropyl propargyl ester takes reaction with Grignard reagents under the metal catalysis, and cyclopropyl allene is finally obtained. The method provided by the invention solves the problems of the existing method that raw materials cannot be easily obtained, the price is high, and the like. The method provided by the invention has the advantages that the raw materials are easy to obtain, in addition, the cyclopropyl is firstly introduced, and various substituent functional groups are then introduced, the variable of the synthesis of various kinds of cyclopropyl allene depends on the aldehyde and the Grignard reagents adopted in the reaction in the last step, and the Grignard reagents are prepared from halogenated hydrocarbon which is cheap and is easy to obtain (the varieties are many), so the method provided by the invention is more suitable for the synthesis of a series of cyclopropyl allene with various substituent groups.

Methods are provided for the catalytic hydroamination of compounds having an alkyne or allene functional group, in which the compound is contacted with ammonia or an amine in the presence of a catalytic amount of a gold complex under conditions sufficient for hydroamination to occur.

The invention discloses a method for synthesizing an indole terpene analogue through Heck / dearomatization cascade reaction, and belongs to the technical field of organic chemistry. Substituted 2-naphthol and N-substituted phenyl allene amine are used as raw materials, and in the presence of a palladium catalyst and a chiral phosphoramidite ligand, Heck / dearomatization cascade reaction is performed to obtain the indole terpene analogue. The method has the advantages of good chemical selectivity and enantioselectivity and high yield, and the product contains a chiral quaternary carbon center.

The invention discloses a method for synthesizing alpha-difluoro methylene phosphonic lactone. In the method, 2,3-allene phosphoni monoester substituted by alpha-difluoro methylene is used as raw material; an iodine cyclizing reagent is added into 2,3-allene phosphoni monoester; an intramolecular iodine cyclizing reaction is performed at normal temperature to obtain alpha-difluoro methylene phosphonic lactone with a six-membered ring structure. After being subjected to recrystallization or column chromatography purification, the prepared phosphonic lactone is expected to become an important enzyme inhibitor. The method is simple and convenient and has high efficiency, mild conditions and high yield. The yield of an aimed compound phosphonic lactone can reach 76 percent to 93 percent.