213 results about "Cyclobutane" patented technology

The radiolabeled non-natural amino acid 1-amino-3-cyclobutane-1-carboxylic acid (ACBC) and its analogs are candidate tumor imaging agents useful for positron emission tomography and single photon emission computed tomography due to their selective affinity for tumor cells. The present invention provides methods for stereo-selective synthesis of syn-ACBC analogs. The disclosed synthetic strategy is reliable and efficient and can be used to synthesize a gram quantity of various syn-isomers of the ACBC analogs, particularly, syn-[18F]-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC) and syn-[123I]-1-amino-3-iodocyclobutane-1-carboxylic (IACBC) acid analogs.

A polymer for ion conductor applications includes a polymer segment having a perfluorocyclobutyl moiety and a polymer segment not having such a moiety. One of these polymer segments is sulfonated to improve ionic conductivity. Fuel cells incorporating the ion conducting polymers are provided.

The invention provides a liquid crystal alignment agent for photo alignment, a liquid crystal alignment layer for photo alignment, and a liquid crystal display element. The liquid crystal alignment agent provided by the invention has a polyamide acid or a derivative thereof, the polyamide acid or the derivative thereof may be formed by reacting a mixer of cyclobutane tetracarboxylic dianhydride or tetracarboxylic dianhydride with specific aromatic diamine of an alkyl chain of a molecule with a carbon number larger than 4. With the adoption of the liquid crystal alignment agent, a liquid crystal alignment layer good in sensitivity of chemical change caused by light irradiation, excellent in alignment property of liquid molecule and high in optical transmittivity is formed. In addition, by applying the photo alignment layer to the liquid crystal display element, the liquid crystal display element with excellent display characteristics can be obtained.

The invention disclosed an aryl nitrile group thiazole derivative for inhibiting the activity of xanthine oxidase, a method for preparing the same and application thereof. In the aryl nitrile group thiazole, R1 is methyl, ethyl, propyl, isopropyl, isobutyl, methyl cyclopropane, methyl cyclobutane, isoamyl, methyl cyclopentane, methyl cyclohexane or aromatic ring methyl, R2 is methyl or trifluoromethyl, and R3 is formic acid, sodium formate, potassium formate, lithium formate, methyl formate, or ethyl formate. Simultaneously, the invention discloses a method for synthesizing the aryl nitrile group thiazole derivative by using inexpensive raw materials, which has the advantages of simple operation, high yield, easy purification of products, application to industrial production and the like, and can obtain an efficient compound with low toxicity through screening; besides, the effective compound is expected to be widely applied to inhibit the activity of the xanthine oxidase required on animals and humans, and to become a new generation of antigout drugs and hyperuricemia drugs with special effect.

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 present invention provides a polyimide precursor of a heat resistant transparent resin substrate material that is excellent in size stability, transparency and heat resistance, can be peeled froma supporting substrate to obtain a thin polyimide film, polyimide and a manufacturing method of a transparent polyimide film. The polyimide precursor has a structural unit originating from diamine, astructural unit originating from acid dianhydride, a structural unit originating from the 2,2'-bi (trifluoromethyl)-4,4'-diaminodiphenyl and a structural unit originating from the 1, 2, 3, 4-cyclobutane tetracarboxylic dianhydride. In all structural units originating from acid dianhydride, more than 70 mol% of structural units originating from 1, 2, 3, 4-cyclobutane tetracarboxylic dianhydride arecontained, and the light transmittance when carrying out the imide operation on the polyimide precursor to form the polyimide, is 5% or less at 308 nm and is 70% or more at 400 nm, and a coefficientof thermal expansion is 45 ppm / K or less.

A process for the production of 4-hydroxybutyraldehyde is described. The process comprises reacting allyl alcohol with a mixture of carbon monoxide and hydrogen in the presence of a solvent and a catalyst comprising a rhodium complex and a diphosphine. The diphoshine is a trans-1,2 -bis(bis(3,4-di-n-alkylphenyl)phosphinomethyl)cyclobutane and / or a 2,3-O-isopropylidene-2,3-dihydroxy-1,4-bis[bis(3,4-di-n-alkylphenyl)phosphino]butane. The process gives high yield of 4-hydroxybutyraldehyde compared to 3-hydroxy-2-methylpropionaldehyde.

The invention provides a novel preparation method of Apalutamide. According to the novel preparation method, 2-fluoro-4-bromo-N-methyl benzene methanamine amide, 1-amino cyclobutyl carboxylate hydrochloride, and the like are taken as initial raw materials, and substitution reaction is carried out so as to obtain 1-((3-fluoro-4-(methyl carbamyl)phenyl)amino) cyclobutane-1-carboxylic acid, wherein synthesis yield is higher than 70%, and purity is higher than 97.2%; then esterification is carried out so as to obtain 1-((3-fluoro-4-(methyl carbamyl)phenyl)amino) cyclobutane-1-carboxylic ester, wherein synthesis yield is higher than 83%, and purity is higher than 97.8%; and at last, ring closing reaction with 2-cyan-3-trifluoromethyl-5-isothiocyano pyridine is carried out so as to obtain Apalutamide, wherein yield is higher than 68%, and purity is higher than 98.1%. The preparation method possesses following advantages: the raw materials are easily available; technology is simple; operationis convenient; yield is high; and cost is low.

The invention discloses a polyimide film as well as a preparation method, a flexible substrate and application thereof. The polyimide is prepared by taking an aromatic dianhydride compound such as 3, 3 minute, 4, 4 minute-biphenyltetracarboxylic dianhydride (sBPDA), cycloaliphatic dianhydride compound 1, 2, 3, 4-cyclobutane tetracid dianhydride (CBDA) or 1, 3-dimethyl-1, 2, 3, 4-cyclobutane tetracid dianhydride (MCBDA) and an aromatic diamine compound as raw materials by virtue of a thermal imidization method. By adjusting the ratio of sBPDA and CBDA or MCBDA, the heat-resisting stability and optical transparence of the polyimide film substrate can be controlled. The film can be used as a flexible substrate to be applied to a flexible display device such as a flexible AMOLED (Active Matrix / Organic Light Emitting Diode), a flexible TFT-LCD (Thin Film Transistor Liquid Crystal Display) and the like.

The present invention provides a curable composition comprising a compound having a single partial structure containing a 4- or more-membered cyclic ether represented by the following formula (I) and a partial structure represented by the following formula (II): wherein in formula (II), R1 represents an alkylene group, a cycloalkylene group or an arylene group, and n represents an integer of 1 to 8.

The object of the present invention is to provide an organosilicon compound having an oxetanyl group, which has a high proportion of an inorganic part in the structure, which, after production thereof, is stable with no gelling, and which has excellent storage stability when it is formed into a composition, and a production method thereof and a curable composition. The organosilicon compound is a compound having an oxetanyl group obtained by a method including a process in which a silicon compound A represented by the formula (1) and a silicon compound B having four siloxane bond-forming groups are subjected to hydrolysis and condensation at a ratio of 0.3 to 2.8 mol of silicon compound B based on 1 mol of silicon compound A.[In the formula, R0 is an organic group having an oxetanyl group, R1 is an alkyl group having 1 to 6 carbon atoms, an aralkyl group having 7 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, or an organic group having an oxetanyl group, X is a hydrolyzable group, and n is 0 or 1.]

The invention discloses a water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex, which has a chemical name of cis-tetrammine-miu-di (3-acetoxy-1, 1-cyclobutane dicarboxylate-O1, O2) dicaryon platinum (II), and can be synthesized by adopting the method preparing the conventional platinum based anti-cancer drug. The anticancer activity of the complex of the invention is higher than the platinum based drug of carboplatin commonly used in clinic, the toxic side effect of the invention is significantly lower than the toxic side effect of carboplatin, and the invention can be made into lyophilized powder or injecta to be used in the clinical cancer treatment.

The invention discloses a cation ultraviolet curing group-containing silicon oxide compound and a preparation method thereof. The preparation method is characterized by comprising the following steps of: mixing and stirring monohydroxy vinyl ether compound or monohydroxy-3-oxetane compound and methoxysilane in the presence of a catalyst in a molar ratio of (1-6)*n:1 until methoxyl group peak disappears in nuclear magnetic resonance spectroscopy; or mixing and stirring monohydroxy olefin compound and the methoxysilane in the presence of the catalyst in a molar ratio of (1-6)*n:1 until the methoxyl group peak disappears in the nuclear magnetic resonance spectroscopy, and then adding the obtained silicon olefin-containing compound dropwise into organic solution of organic peracid for performing epoxidation, wherein the number n of siloxicon bonds in molecules is an integer of 2 to 4. The preparation method has the advantages of low cost and readily available raw materials, simple and convenient preparation operation and convenient industrial production; and the obtained cation ultraviolet curing group-containing silicon oxide compound can be cured rapidly by ultraviolet irradiation; and the obtained coating has the advantages of high smoothness, high flame retardant efficiency and wide industrial application prospect.

A photoalignment agent includes: a copolymer obtained from at least one of cyclobutane dianhydride (CBDA) and a cyclobutane dianhydride derivative, and a diamine; and a cross-linking agent including an alkylene group —CnH2n—, n being a natural number.

A medicine of Pululishaxing is prepared by: using 4-bromomethyl-5-methyl 1,3-dioxacycloene pentadione as start material, addition reacting with piperazine to produce 5-methyl-4-piperazinemethyl-1,3-dioxacycloenepentenedione, finally, reacting with 6,7- difluoro -1- methyl - 4 -oxo-4-[1,3]thioaza cyclobutane [3,2 -a] quinoline-3- carboxylic acid. The process is simple, high purity, high yield. Their purity of crude product can reach 97.5% more. Yield of the product is more than 58%, increased 45% compared with prior art. It is proficial.

The invention provides an environment-friendly chlorofluorocarbon-free refrigerant and a preparation method thereof. The refrigerant is prepared from propane, propylene, cyclobutane, 2,3,3,3-tetrafluoropropene, trans-1,3,3,3-tetrafluoropropene, trifluoromethyl iodide, pentafluoromethyl iodide, difluoromethane, tetrahydrothiophene, liquid carbon dioxide and cryogenic lubricant. The refrigerant has the beneficial effects that the ODP value is zero, the ozone sphere cannot be destroyed if the refrigerant is used for a long time; the GWP value of raw materials is low, and the working pressure of the refrigerant is equivalent to that of R22, so that an existing refrigeration system need not to be modified, the production cost can be reduced, while the refrigeration effect is not reduced; the refrigerant has the effects of inhibiting combustion and explosion, so that the combustibility of the refrigerant can be reduced, and the safety can be improved; the lubricant can seep into each part of a compressor together with the refrigerant so as to create an excellent condition for engine lubrication; tetrahydrothiophene is easily dissolved in difluoromethane and has a strong unpleasant smell, so that when the refrigerant leaks, a user can feel leakage of the refrigerant at the first time and carries out corresponding measures, so that property and safety of people can be protected.

Provided is a monomer composition that has rapid curability and can be cured rapidly, even in the presence of oxygen and / or water, to form a cured product having excellent adhesion to a wide variety of substrates. The monomer composition according to the present invention contains a vinyl ether compound (A). The vinyl ether compound (A) includes a vinyl ether compound (a) having a cyclic ether skeleton. The monomer composition further contains at least one compound selected from the group consisting of a vinyl ether compound (a′) having a chain hydrocarbon skeleton, a divinyl ether compound (a″-1) having a cyclic hydrocarbon skeleton, an oxetane compound (B), and an epoxy compound (C).

A process for preparing α, ω-functional siloxane compounds in a purity of greater than or equal to 90% includes contacting a monohydrosiloxane compound of formula 1 with oxygen in the presence of a platinum group catalyst, without adding water, to form the α, ω-functional siloxane compound in a purity of greater than or equal to 90%; wherein n is 0, 1, or 2; R1 is fluoroethyl, methyl or phenyl; and R2 is substituted alkyl, epoxyalkyl, oxetanylalkyl, substituted oxaalkyl, epoxyoxaalkyl, oxetanyloxaalkyl, alkenyl, alkylalkoxysilyl, substituted alkylaryl, and substituted arylalkyl.

The invention relates to new type precursor compounds for preparing platinum carrying catalyst [Pt(NH3)4]X2(X2=oxalate, malonate and 1, 1-cyclobutanes dicarboxylate), and a method for making same. The compounds can provide complex cation [Pt(NH3)4]<2+>, is propitious to perform high-performance catalyst on carrier or sodium-typed molecular sieve for adsorbing and exchanging electrified negativity. The preparation of the compounds uses K2PtCl4 as starting material to obtain the intermediate body cis-[Pt(NH3)2I2] by iodination and ammine substitution, and then to obtain the target compounds after hydration, coordination and ammine displacement, and the yield can reach 90.

The invention discloses a method for synthesizing dicycloplatin by microwave catalysis. The method comprises the steps: mixing carboplatin and 1,1-cyclobutane dicarboxylic acid in a corresponding ratio as well as a solvent; according to a molar ratio of the carboplatin to the 1,1-cyclobutane dicarboxylic acid of 1:(1 to 1.5), performing a reaction for 9 minutes in microwaves, controlling a temperature of 30 DEG C, then carrying out decompressing condensing at a temperature of 35 DEG C, washing a filter cake with ethyl alcohol, and after vacuum drying, obtaining the dicycloplatin. The method disclosed by the invention has the advantages of convenience for operation, mild reaction condition, short reaction time, high reproducibility ad high product purity.

The invention relates to a preparation method of diaminomethyl cyclobutane oxalate, which comprises the following steps: carrying out dimerization on acrylonitrile used as a raw material to generate a cis-dinitrile cyclobutane / trans-dinitrile cyclobutane mixture, carrying out distillation separation on the generated cis-dinitrile cyclobutane / trans-dinitrile cyclobutane mixture, and converting into trans-dinitrile cyclobutane by reduction; by using active nickel as a catalyst, introducing ammonia, and pressurizing with hydrogen to react, thereby obtaining trans-diaminomethyl cyclobutane; adding oxalic acid to obtain a crude diaminomethyl cyclobutane oxalate product; and finally, purifying with alcohol to obtain the finished diaminomethyl cyclobutane oxalate product. By using the method provided by the invention, the raw material is accessible, the operation is easy to control, the obtained product can be used as an intermediate to participate in the synthesis of Lobaplatin, and the obtained Lobaplatin has more stable properties and is more suitable for industrial production.

The invention belongs to the field of organic synthesis and discloses a method for synthesizing trans-3-hydroxy cyclobutyl formic acid. The method comprises the following steps: by using an appropriate reducing agent, reducing 3-carbonyl-cyclobutane formate (C1-C6 alkyl ester) into single trans-3-hydroxy cyclobutyl formic ether in an efficient stereoselectivity manner, and further performing a Mitsunobu reaction and hydrolysis, thereby obtaining single trans-3-hydroxy cyclobutyl formic acid. The method provided by the invention is high in synthesis method raw material availability, mild in reaction condition, good in stereoselectivity and relatively high in yield; in addition, aftertreatment and purification are both easy to operate, and the method is applicable to industrial amplified production.

The invention relates to a novel water-soluble platinum (II) anticancer complex, a leaving group of which is 3-acetoxy-1 and 1-cyclobutane dicarboxylate root (3-COO-CBDCA), and a carrier of which is an ammonia / amine ligand of a listed platinum antitumor drug. The carrier comprises ammonia (NH3), 1R, 2R-diamino cyclohexane (DACH), 1,2-bis (aminomethyl)-cyclobutane, 2-isopropyl-(4R, 5R)-4, 5-bis (aminomethyl)-1 and 3-dioxo-cyclopentane. The novel water-soluble platinum (II) anticancer complex can be synthesized by the normal preparation method of the platinum antitumor drug. The antitumor activity of the complex is equivlent to that of the prior carboplatin frequently used in clinic, and the toxicity and side-effect of the complex are obviously less than those of carboplatin, can be made into freeze-dried powder or injection for cancer treatment in clinic.

The present invention relates to a new kind of water soluble anticancer Pt (II) compound, cis-[2-substitutent- (4Rú¼5R)-4ú¼5-bis(aminoethyl)-lú¼3-dioxycyclopentaneíñ3-hydroxy-1ú¼1-cyclobutane dicarboxylic radical- Pt (II)], with the substitutent being methyl, ethyl or isopropyl radical. One of the preparation process includes the reaction of material cis-[PtA2I2], with A2 being 2-substitutent- (4Rú¼5R)-4ú¼5-bis(aminoethyl)-lú¼3-dioxycyclopentane, and 3-hydroxy-1ú¼1- cyclobutane dicarboxyl-Ag, filtering to separate AgI, concentrating the mother liquid and freeze drying to obtain the coarse product. The other preparation process includes the first reaction of cis-[PtA2I2] and Ag2SO4, filtering to separate AgI, the reaction of the mother liquid and 3-hydroxyl-1ú¼1-cyclobutane dicarboxylic Ba, filtering to separate BaSO4, concentrating mother liquid, and freeze drying to obtain the coarse product. The coarse product is re-crystallized in water / alcohol system to obtain refined product. The compound of the present invention has anticancer activity and less toxic side effect, and may be clinical use for treating cancers.

Ulifloxacin has low water solubility and low bioavailability. The invention relates to an Ulifloxacin salt, a preparation thereof, a kit having the medicinal antibiotic preparation and the use of the new Ulifloxacin salt in the preparation of an anti-bacterial-infection medicine. The invention particularly relates to a new medicinal preparation which is used for injection and can be stored stablyand the chemical name of which is 6-fluoro-1-methy-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiazeto[3,2-alpha]quinoline-3-carboxylate. In the invention, the medicinal preparation is administrated by direct injection in form of thiabutyldine quinoline carboxylate, the solubility is improved, the bioavailability is improved and treatment effect is enhanced.