352 results about "Pinacol" patented technology

The invention discloses a method for preparing crisaborole and an intermediate for preparing crisaborole. The method comprises the following steps: (1) enabling components such as 2-halogen-5-(4-cyanphenoxy) benzyl acetate and bis(pinacolato)diboron to react in the presence of an organic solvent and a palladium catalyst under an alkali condition so as to obtain components such as 2-acetoxyl methyl-4-(4-cyan phenoxy) phenylboronic acid pinacol ester; (2) enabling components such as the 2-acetoxyl methyl-4-(4-cyan phenoxy) phenylboronic acid pinacol ester to react in a solvent under an acid oralkali condition, thereby obtaining crisaborole. The method is gentle in reaction condition, easy to operate, high in reaction yield, simple in aftertreatment, relatively low in cost and applicable toindustrial production.

The invention provides a method for preparing baricitinib. The method comprises the following steps: by taking 4-pyrazol boric acid pinacol ester (10) as an initial raw material, performing Michael addition reaction on the initial raw material and 3-(icyanomethylene) azacyclo-cyclobutane-1-tert-butyl formate (11) so as to prepare an intermediate 12, and performing catalytic coupling reaction on 12 and 13, thereby preparing an intermediate 14; removing two-molecule tert-butyl formate of the intermediate 14, thereby preparing an intermediate 15; performing sulfamide reaction on the intermediate 15 and ethanesulfonyl chloride in an organic solvent, thereby obtaining a final product baricitinib (1). The method for preparing baricitinib has the advantages that the raw materials are easy to obtain, the process is simple, the operation is convenient, the reaction yield is high when being compared with that of document records, the atom utilization rate is high, industrial production can be easily achieved, and the like. The reaction general formula is as shown in the specification.

The invention provides an electrolyte, a positive electrode, a preparation method thereof, and a lithium ion battery. The electrolyte comprises lithium salts, an electrolyte solvent, and an additive. The additive is boric acid pinacol ester provided by the invention. The electrolyte has the advantages that boric acid pinacol ester is taken as the special additive, can protect the positive electrode, and at the same time, protects the electrolyte solvent from being oxidized and decomposed under a high potential so as to avoid excess consumption. The service life of battery is prolonged under a high voltage.

Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-19-nor-(20S)-1α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and / or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cis-retinoic acid, all-trans-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid, 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-napthoic acid, 4-[1-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t-butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and / or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.

The invention belongs to the field of organic chemical synthesis and provides a synthetic method of 1-alkylpyrazole-4-boronic acid pinacol ester. The synthetic method comprises the following three steps: 1. reacting pyrazole with iodine and hydrogen peroxide to generate 4-iodopyrazole A; 2. reacting the 4-iodopyrazole with alkyl halide to obtain an intermediate B; 3. preparing a Grignard reagent of the raw material by using 1-alkyl-4-iodopyrazole as a raw material and adopting an isopropyl Grignard reagent exchange method at 0-30 DEG C, with BE001 as a boron reagent, and reacting to obtain the final product. The technological method is accessible in raw materials, simple and convenient to operate and lower in cost and is a proper method for preparing 1-alkylpyrazole-4-boronic acid pinacol ester compounds.

According to the method of the present invention, a methyl tetrazole pyridine bromide (2) and pinacol diboron are subjected to a reaction under catalysis of a transition metal to obtain a boronic acid pinacol ester (3), the compound (3) is separated or is not separated, and the separated compound (3) or the un-separated compound (3) and Cbz-protected bromobenzene (4) are subjected to a reaction under catalysis of a transition metal to obtain a key intermediate (1) of tedizolid. According to the present invention, the compound (3) is not subjected to separation purification, and reacts with the compound (4) in a kettle to generate the compound (1).

The invention discloses a mazarine electroluminescent compound, and a preparation method and application thereof. The mazarine electroluminescent compound has a structure as shown in a formula I which is described in the specification. In the formula, X is O or S; R1 is H, halogen, a cyano group, an alkyl group, an alkyloxy group or a phosphate radical; and R2 is H, a diphenylphosphine oxide radical, a diphenylamino group or a carbazolyl group. The compound as shown in the formula I is prepared by preparing a dibenzofuran(or dibenzothiophene)-4-pinacol borate precursor and a phenanthroimidazole precursor at first and then carrying out a coupling reaction. The preparation method for the compound is easy to operate and has high yield; the compound has mazarine fluorescence and good monochromaticity; and an OLED device prepared with the compound as a luminescent material has mazarine emission, starting voltage of 3.6 V and maximum external quantum efficiency of 1.63%.

The invention provides a novel method for synthesizing N-tert-butoxycarbonyl-1,2,5,6-tetrahydropyridine-4-boronic acid pinacol ester, which belongs to the technical field of chemical synthesis. The method comprises the following steps of: obtaining a target product, namely the N-tert-butoxycarbonyl-1,2,5,6-tetrahydropyridine-4-boronic acid pinacol ester through a three-step reaction by taking N-(tert-butoxycarbonyl)-4-piperidone, 4-aminopyridine, trifluoromethanesulfonic anhydride, n-butyl lithium, bis(pinacolato)diboron, triethylamine, diisopropylamine and potassium acetate as raw materials,dichloromethane, tetrahydrofuran and dioxane as solvents, and [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II) as a catalyst; and characterizing data through liquid chromatogram, nuclear magnetic spectrum and mass spectrum. By the method, the production period is short, the synthetic cost is low, a synthetic process is safe and reliable, and a post-treatment method is simple, convenient and quick; and the yield of a product is high (51 to 58 percent) and the purity of the product is high (98.2 to 99.6 percent).

The invention discloses a dendritic hyperbranched polymer as well as a preparation method and a use thereof. The structural formula of the polymer is shown in the specification, wherein R is a low-algebraic dendritic macromolecule based on azobenzene chromophore. The dendritic hyperbranched polymer is prepared through substitution reaction, click chemical reaction and suzuki reaction of 9-(6-azidohexyl)-3,6-dibromocarbazole, triphenylamine tri-band pinacol cyclic ester as well as the low-algebraic dendritic macromolecule based on azobenzene chromophore. The polymer disclosed by the invention is gentle in polymerization reaction conditions, high in yield, large in molecular weight and low in degree of dispersion. The polymer disclosed by the invention has good second-order nonlinear optical performance and thermal stability, and can be used as a second-order nonlinear optical material for being practically applied in the aspects of remote communication, data storage, data conversion, phase conjugation, signal modulation and the like.