734 results about "Phenacyl" patented technology

A fragrance delivery system which releases fragrant alcohols upon exposure to light. The system comprises 2-benzoyl benzoates of general formulae which can comprise various subtituents R1-R5 as defined in the application and a substituted R* which is the organic part of a fragrant alcohol.

A method for classifying cancer patients as eligible to receive cancer therapy with a small molecule inhibitor of Bcl-2 comprising determination of the presence or absence in a patient tissue sample of chromosomal copy number status at the chromosomal locus 13q14 comprising the microRNA's miR-15a and miR-16-1 or at the chromosomal locus 11q23.1 comprising the microRNA miR-34c. The classification of cancer patients based upon the presence or absence of 13q14 loss or gain allows better selection of patients to receive chemotherapy with a small molecule Bcl-2 inhibitor such as N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl) methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl) methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide, and for monitoring patient response to this therapy.

An alkyl substituted triazazole type antifungal compound for preparing the antifungal medicines, and its various enantiomers, diaisomers, Nox and precursors are disclosed.

A crystal form of folic acid antagonistic N-(4-(2-(2-amino-4,7-methyl-4-oxo-1H-pyrrolo(2,3-d)pyrimidine-5-radical)ethyl)benzoyl)-L-glutamic acid disodium salt and its production are disclosed.

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

The invention discloses substituted-evodiamine anti-tumor and antifungal compounds and a preparation method thereof. The compounds have a general structural formula (I), wherein R represents: (1) benzyl or substituted benzyl; (2) benzoyl or substituted benzoyl; (3) linear or branched alkyl having 2 to 6 carbon atoms; and (4) an ester group. The substituted-evodiamine compounds of the invention have good anti-tumor activities for various tumor cells, provide a new way for deep research and development of new anti-tumor medicaments and can be used for preparing new anti-tumor medicaments.

The invention discloses a novel compound and a preparation method and use thereof. The novel compound is represented by a formula A, wherein R is selected from THP (trtrahydropyranyl), trialkyl silicon-base, acetyl, benzoyl and biphenyl formoxyl.

A positive photosensitive composition comprises: (A) an acid generator capable of generating an acid upon irradiation with one of an actinic ray and a radiation; and (B) a resin having a monocyclic or polycyclic alicyclic hydrocarbon structure and capable of decomposing by the action of an acid to increase the solubility in an alkali developer, wherein the acid generator (A) comprises at least two compounds of a sulfonium salt compound not having an aromatic ring, a triarylsulfonium salt compound, and a compound having a phenacylsulfonium salt structure.

The invention provides a preparation method of 3,5-dibenzoyl-2-deoxy-2-fluoro-2-methyl-D-ribo-gamma-lactone (sofosbuvir). The method comprises the following steps: adding alkali into a mixed solution of L-alanine isopropyl ester or an acid salt thereof and phenyl dichlorophosphate for reacting to obtain (S)-2-phenoxy-chloro-phosphoryl amino isopropyl propionate, reacting the (S)-2-phenoxy-chloro-phosphoryl amino isopropyl propionate with 4-trifluoromethylphenol in the presence of alkali at the temperature of 0-10 DEG C to obtain racemic (S)-2-[(4-trifluoromethyl-phenoxyl)-phenoxy-phosphoryl amino)]alanine isopropyl ester, dissolving the racemic (S)-2-[(4-trifluoromethyl-phenoxyl)-phenoxy-phosphoryl amino)]alanine isopropyl ester into an ether or alkane solvent at the normal temperature, cooling to 50-10 DEG C below zero, and separating (S)-2-[(S)-(4-trifluoromethyl-phenoxy)]-phenoxy-phosphoryl amino)]alanine isopropyl ester out; and reacting the (S)-2-[(S)-(4-trifluoromethyl-phenoxy)]-phenoxy-phosphoryl amino)]alanine isopropyl ester with (2'R)-2'-deoxy-2'-fluoro-2'-methyluridine in the presence of organic alkali with high steric hindrance to obtain the 3,5-dibenzoyl-2-deoxy-2-fluoro-2-methyl-D-ribo-gamma-lactone. The method has the advantages of simple steps, mild reaction and suitability for industrial production.

The instant disclosure provides crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, salts and solvates thereof. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form(s), as well of methods of using the crystalline form(s) in the treatment of HIV and / or AIDS, and methods for obtaining such crystalline form(s).

This present disclosure is related to the field of 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Fungicides are compounds, of natural or synthetic origin, which act to protect and / or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less. The present disclosure relates to 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-one compounds and their use as fungicides. The compounds of the present disclosure may offer protection against fungi and fungi like organisms including ascomycetes, basidiomycetes, deuteromycetes, and oomycetes.

The invention belongs to the field of organic synthesis, and discloses a preparation method of 3-hydroxy-substituted pyrazol as shown in the formula (I). The response equation is : (a chemical formula), and definition of each substituent group in the formula is shown in a instruction book. Substituted benzene formoxyl ethyl carboxylic acid ester as shown in the formula (II) and substituted hydrazine as shown in the formula (III) serve as raw materials, simultaneously the substituted hydrazine as shown in the formula (III) serves as a solvent, and reaction is carried out at 0-40 DEG C for 5-10 hours. When the substituted hydrazine with low concentration is adopted, inorganic salt is added in a reaction system, and charging ratio of (II), (III) and the inorganic salt is 1: (3-10): (0-1). The preparation method is easy in raw material acquisition, simple in synthetic route, simple and convenient in operation, high in product yield, easy to purify and the like, and applicable to laboratory synthetics and industrial production.

Disclosed are: a novel orange-colored disperse dye which has excellent staining properties onto a hydrophobic fiber material, a high light-resistant color-fastness, an excellent sublimation fastness, and a good buildup property, and is useful as a dye for use in an automotive interior sheet; a disperse dye composition for yellow-to-orange, brown, dark blue and black colors which comprises the disperse dye; an ink for ink-jet printing; a staining method or a stained material using the disperse die, the composition or the ink. The orange-colored disperse dye is represented by the formula (1) below and can stain a hydrophobic fiber material (e.g., a polyester) into orange color. [Chemical formula] (1) wherein X1 represents a chlorine or bromine atom; R1 represents a benzoyl group, a cyanoethyl group, a C1-C4 alkyl group, a phenyl group or a phenyl group substituted by at least one C1-C4 alkyl group.

In the method of the present invention a plastic article (e.g., a molded article of thermoplastic polycarbonate) is immersed at least partially in a dye bath which includes one or more dyes, water, at least one carrier, and at least one diol. The dye bath contains: (i) at least one dye (e.g., a static and / or photochromic dye); (ii) water; (iii) at least one carrier represented by the following general formula I, R—O—(CH2)n—OH   I wherein R is a radical selected from linear or branched C1-C18 alkyl, benzyl, benzoyl and phenyl, and n is 2 or 3; and (iv) a diol selected from at least one of linear or branched C2-C20 aliphatic diols, poly(C2-C4 alkylene glycol), cycloaliphatic diols having from 5 to 8 carbon atoms in the cyclic ring, monocyclic aromatic diols, bisphenols and hydrogenated bisphenols. In an embodiment of the present invention, the carrier is ethyleneglycol butyl ether, and the diol is diethylene glycol. The present invention also relates to a method of separating the dye from the water, carrier and diol components of the dye bath, by contacting the dye bath with particulate activated carbon.

The object of the present invention is to provide an optical film excellent in transparency, heat resistance and processability. An optical film containing a polymer having at least a repeating unit represented by following general formula (I):wherein in the general formula (I), R1 and R3 each independently denote a hydrogen atom, a straight-chain or branched alkyl group with a carbon number of 1 to 4, or a substituted or unsubstituted phenyl group; R2, A and B each independently denote a hydrogen atom, a halogen atom, a straight-chain or branched alkyl group with a carbon number of 1 to 4, a straight-chain or branched alkyl halide group with a carbon number of 1 to 4, a straight-chain or branched alkoxy group with a carbon number of 1 to 4, an alkoxycarbonyl group, an acyloxy group, an amino group, an azide group, a nitro group, a cyano group or a hydroxyl group (however, R2 is not a hydrogen atom); R4 denotes a hydrogen atom, a straight-chain or branched alkyl group with a carbon number of 1 to 4, a substituted or unsubstituted cycloalkyl group with a carbon number of 5 to 10, a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, or a substituted or unsubstituted heterocyclic group; R5 denotes a hydrogen atom, a straight-chain or branched alkyl group with a carbon number of 1 to 4, a benzyl group, a silyl group, a phosphoric acid group, an acyl group, a benzoyl group or a sulfonyl group; l, m and n denote an integer of 2 or more.

The invention relates to a preparation method of di (2,4,6-trimethylbenzoyl) phenyl phosphine oxide and (2,4,6-trimethylbenzoyl) diphenyl phosphine oxide used in the technical field of radiation polymerization curing new materials, hydrogen phosphide as a raw material is reacted with chlorobenzene or bromobenzene and 2,4,6-trimethylbenzoyl chloride, and an acyl oxygen phosphonic compound is obtained by oxidizing with an oxidant. By adjusting the feed ratio, the di (2,4,6-trimethylbenzoyl) phenyl phosphine oxide and the (2,4,6-trimethylbenzoyl) diphenyl phosphine oxide are respectively obtained, and the purpose for simultaneously producing the two target products of di (2,4,6-trimethylbenzoyl) phenyl phosphine oxide and the (2,4,6-trimethylbenzoyl) diphenyl phosphine oxide can be achieved by use of same material and device, and compared with known technology paths reported in literatures, the preparation method has the significant advantages of novelty of the chemical reaction technology, cost economic competitiveness and environmental friendliness.

The invention is a kind of 2-pyrimidine oxo-N-urea phenyl benzyl amine compound, the manufacturing method. The structural formula is shown in the picture. D or E = hydrogen, halogen, C1-4C alkyl, C1-C4 alkoxy, C1-C4 halogenated alkyl or C1-C4 alkylogen oxide; X=hydrogen, halogen, nitro, cyan, carboxy, ester group, sulfonyl, C1-C8 alkane acyl amido, C1-C8 halogeno alkane acyl amido, C1-C8 alkane acyl group, C1-C8 alkyl, C1-C8 halogeno alkyl, C1-C8 alkoxy, phenyl etc; R1, R2=hydrogen, ester group, sulfonyl, C1-C8 alkyl, C1-C8 substituted alkyl, C1-C8 alkyl acyl, phenyl, etc; Xí» is H, urea, halogen atom, carboxy, ester group, C1-C8 alkane acyl, C1-C8 alkyl, C1-C8 halogeno alkyl, C1-C8 alkoxy, phenyl, substitution phenyl or heterocyclic radical; R3=hydrogen, C1-C8 alkane acyl, C1-C8 halogeno alkyl, benzene formyl, substitution benzene formyl, C1-C8 alkyl.

The related preparation method in hydrosolvent for N-[4-]2-(2-amido-4, 7-dihydro-4-oxo-3H- pyrrolo[2, 3-d]pyrimidine-5-radical)ethyl]benzoyl]-L-glutacid (Pemetrexed) and its acceptable salt in pharmacy is to react the 4-[2-(2-amido-4, 7-dihydro-4-oxo-3H-pyrrolo[2, 3-d] pyrimidine- 5-radical)ethyl]benzoic acid with L-glutacid dissolved in organic solvent and water. This invention is more simple than prior art and fit to industrial production.

In the method of the present invention a plastic article (e.g., a molded article of thermoplastic polycarbonate) is immersed at least partially in a dye bath which includes one or more dyes, water, at least one carrier, and at least one diol. The dye bath contains: (i) at least one dye (e.g., a static and / or photochromic dye); (ii) water; (iii) at least one carrier represented by the following general formula I,R—O—(CH2)n—OHIwherein R is a radical selected from linear or branched C1–C18 alkyl, benzyl, benzoyl and phenyl, and n is 2 or 3; and (iv) a diol selected from at least one of linear or branched C2–C20 aliphatic diols, poly(C2–C4 alkylene glycol), cycloaliphatic diols having from 5 to 8 carbon atoms in the cyclic ring, monocyclic aromatic diols, bisphenols and hydrogenated bisphenols. In an embodiment of the present invention, the carrier is ethyleneglycol butyl ether, and the diol is diethylene glycol. The present invention also relates to a method of separating the dye from the water, carrier and diol components of the dye bath, by contacting the dye bath with particulate activated carbon.

A process for the preparation of taxanes comprising wherein R is a tert. butoxycarbonyl or benzoyl group; PMP is p-methoxyphenyl group; G1 is acetyl group; G2 is haloacetyl group comprisinga) protecting the C-7 hydroxyl group of 10-deacetylbaccatin III with haloacetyl chlorides and then acetylating the C-10 hydroxyl group with acetyl chloride to obtain a protected 10-deacetylbaccatin III (1);b) subjecting the protected 10-deacetylbaccatin III (1) to coupling with an oxazolidine-5-caboxylic acid of formula 2 wherein R is tert. butoxycarbonyl or benzoyl; PMP is p-methoxyphenyl group in the presence of a condensation agent and an activating agent to obtain C-13 esters of formula 3;c) treating the coupled products 3 with weak acidic medium to open the oxazolidine ring to obtain intermediates of formula 4; wherein R is a tert. butoxycarbonyl or benzoyl group; G1 is acetyl group; G2 is haloacetyl groupd) subjecting the intermediates of compound 4 to selective deprotection of haloacyl group in the presence of acetyl group under mild alkaline condition at −20 to +40° C. for 6-24 h in the presence of ammonia or aliphatic amine or aromatic amines or their combination to obtain paclitaxel or docetaxel.

In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon. The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.

The invention provides a method for preparing a chlorinated 2-benzoyl-1,10-phenanthroline condensed amine iron (II) complex shown in formula I, and its catalytic application in ethylene oligomerization. The preparation method comprises the following steps: orderly performing hydrolysis and an oxidation reaction with nitrobenzene of initial reaction raw materials of 1,10-phenanthroline and benzyl lithium to obtain 2-benzoyl-1,10-phenanthroline, then performing condensation of 2-benzoyl-1,10-phenanthroline with substituted aniline to obtain 2-benzoyl-1,10-phenanthroline condensed amine ligand, and reacting the ligand with ferrous chloride to obtain a target product I. The synthetic method provided by the invention is few in steps, and simple in process, substitutes nitrobenzene for selenium dioxide in the prior art for the oxidation reaction, substitutes nontoxic benzyl lithium for hypertoxic potassium cyanide in the prior art, reduces the preparation cost of the catalyst, and has wide industrialization prospects.

The invention belongs to the field of high-molecular materials, in particular to bromo-polyarylether ketone / polyarylether sulphone the phenmethyl position of which is substituted by bromine and a preparation method thereof. The bromo-polyarylether ketone / polyarylether sulphone is prepared by taking tetramethyl-diphenol type polyarylether ketone (polyarylether sulphone) containing phenacyl as a polymer main body and N-bromosuccinimide as raw materials and introducing a bromine group to the main chain of the polymer. The bromination degree can be effectively controlled by regulating reaction time and the ratio of monomer to the polymer, laying foundations for further functionalizing the polymer. Meanwhile, the introduction of a polar functional group can reduce crystals of the polymer, thereby effectively improving the processability of the polymer.

The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is -C(O)O-C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).