690 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.

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.

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.

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 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).

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.

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 comprising

• • a) 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 group

d) 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).

The invention relates to a mangiferin aglycon derivative which has the chemical structure shown as in the chemical structure general formula (I), wherein R1, R2, R3 and R4 are selected from a, b, c or H, and R1, R2, R3 and R4 can not be H simultaneously; a refers to propionyl, butyryl or valeryl, b reters to various substituted benzoyl groups, and c refers to various substituted phenylsulfonyl groups. The invention also provides a preparation method and an application of the mangiferin aglycon derivative. The advantages are as follows: the compound has good blood glucose lowering effect whichis obviously superior to that of mangiferin and mangiferin aglycon, and the compound has no influence to blood glucose and blood fat of a normal rat and no toxic-side effect exist. The preparation method of the compound is convenient and feasible and has good repeatability and high compound yield; and with good officinal effect, the compound can be used for preparing drugs for treating diabetes mellitus and has wonderful development and utilization values. Formula (I).

The invention discloses a preparation method of phenyl bis(2,4,6-trimethylbenzoyl)phosphine oxide as an efficient free radical photoinitiator. The preparation method of phenyl bis(2,4,6-trimethylbenzoyl)phosphine oxide comprises the concrete steps of with 2,4,6-trimethylbenzaldehyde as a raw material, enabling 2,4,6-trimethylbenzaldehyde and phenylphosphine oxide to be subjected to condensation reaction in the existence of a catalyst, and then, carrying out oxidation reaction. Extraction and solvent replacement are not needed and continuous reaction can be realized in the reaction process. The preparation method of phenyl bis(2,4,6-trimethylbenzoyl)phosphine oxide, disclosed by the invention, is low in price, environment-friendly, easy to operate and suitable for realizing industrialization.