487 results about "Benzylamine" patented technology

The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.

A composite herbicide for rape field contains the pyrimidine benzylamine kind of herbicide, at least one of quizalofop-ethyl, fluazifop-p-butyl, haloxyfop, fenoxaprop and sethoxydim, acetochlor, alachlor, napropamide, ehaprochlor, metolachlor, ethamet sulfuron and benazolin. Its advantages are high effect, broad spectrum, low dosage and high safety.

The present invention describes methods of treating dementia comprising administering an effective daily dose of N-(2-(6-fluoro-1H-indol-3-yl)ethyl-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.

This invention relates to the use of 4-amidino benzylamine derivatives as cosmetic ingredients and to cosmetic compositions, as well as to non-therapeutic methods for the cosmetic treatment of the skin and the scalp. Said derivatives and compositions can be used as urokinase inhibitors to prevent and restore damage of the epidermal barrier. Barrier abnormalities and disruptions respectively are often the starting point of a dry skin state, of itching, of dandruff and of the perception of sensitive skin. These 4-amidino benzylamine derivatives can be used for topical skin and scalp care applications in form of creams, lotions, gels, shampoos and the like.

The invention relates to an intermediate of pemetrexed disodium, a preparation method thereof and a method for preparing pemetrexed disodium thereby; and the intermediate is (2-(4-(3-(2,4-diamino-6-oxy-1,6-dihydro-pyridine-5-group)-3-(1,3)dioxolane-2-group-propyl) benzylamine)sodium glutaric acid. The synthesis of the intermediate comprises the following steps: firstly, condensation reaction is conducted on 4-bromobenzoic acid or 4-iodobenzoic acid and L-glutamate diethylester, then Hack reaction is conducted, 4-bromo is replaced and 4-butyraldehyde is formed, then selective bromo replacement is conducted and the 4-butyladehyde is converted into 2-bromobutyraldehyde, and then condensation reaction of aldehyde and ethylene glycol is utilized for protecting the aldehyde, and pyrimidine ring is further synthesized, and finally the intermediate is obtained. Acid hydrolysis ring-closing reaction and sodium hydroxide salification are respectively conducted for once on the intermediate so as to obtain the pemetrexed disodium. The method for preparing pemetrexed disodium in the invention has high yield, low cost and easy operation and is applicable to industrialized production.

The present invention provides a method for preparing 1,3-dibenzylimidazoline-2-ketone-cis-4,5- dicarboxylic acid, and is characterized by that it utilizes chlorine gas to make fumaric acid produce electrophilic addition reaction to obtain meso-2,3-dichlorosuccinic acid, in the pressence of phase transfer catalyst the meso-2,3-dichlorosuccinic acid and benzylamine are undergone the processes of benzylamination reaction in the solvent so as to synthesize cis-2,3-dibenzylamine succinic acid, the latter and solid carbonyl chloride and undergone the process of phase transfer catalytic ring-closing reaction in the potassium hydroxide solution so as to obtain the invented product. Its total yield rate is up to 74%.

The invention discloses a polyurethane sealant and a preparation method thereof. The polyurethane sealant comprises 30-70 weight percent of performed polymer, dinonyl phthalate, carbon soot, N,N-dimethyl benzylamine, byk-111, oxazolidine, epoxy silicone hydride and amino-group silicone hydride, wherein the performed polymer is obtained through the reaction of polyoxyalkylene dihydric alcohol, polyoxypropylene trihydric alcohol, hexamethylene glycol and 4,4'-diphenylmethane diisocyanate by taking dibutyl tin laurate as a catalyst. After being solidified, the polyurethane sealant has over 8MPa of tensile strength of elastomer and over 450 percent of elongation at break, not only has better solidifying speed at normal temperature, but also has very high solidifying speed at low temperature and low humidity. The polyurethane sealant is suitable for elastic splicing with high mechanical property, such as the elastic splicing during the installation of glass of automobiles, trains, ships, airplanes, cable cars, and the like and is suitable for the rapid splicing at low temperature and low humidity and other elastic splicing with high mechanical property.

A new method of ortho-fluorination where an aryl C—H bond is directly replaced by an aryl C-F bond in a palladium-catalyzed reaction is provided. The method includes the ortho-fluorination of a triflamide protected benzylamine, a palladium catalyst, such as Pd(OTf)₂, a fluorinating reagent such as N-fluoro-2,4,6-trimethylpyridinium triflate, and a ligand to promote the reaction such as N-methylpyrrolidinone (NMP).

The invention discloses a liquid-phase synthesis method of dipeptide diaminobutyroyl benzylamide diacetate. The method comprises the following steps of enabling Boc-Beta-Ala-OH, N-ethyl-5-phenylisoxazole-3'-sulfonic acid inner salt and H-Pro-OMe.HCl to react to obtain Boc-Beta-Ala-Pro-OMe, and enabling the Boc-Beta-Ala-Pro-OMe to react with LiOH to obtain Boc-Beta-Ala-Pro-OH; afterwards, synthesizing Boc-Beta-Ala-Pro-DAB(Boc)-OH with the Boc-Beta-Ala-Pro-OH and H-DAB(Boc)-OMe.HCl by adopting the same method; next, enabling the Boc-Beta-Ala-Pro-DAB(Boc)-OH, 1-hydroxybenzotriazole, N,N-diisopropylcarbodiimide and benzylamine to react to obtain Boc-Beta-Ala-Pro-DAB(Boc)-NH-Bzl, finally, removing a Boc protecting group by using trifluoroacetic acid, separating and purifying, so as to obtain the dipeptide diaminobutyroyl benzylamide diacetate with purity being more than 95 percent. According to the liquid-phase synthesis method, amino acid methyl ester which is low-cost and is easily obtained is used as a raw material; a by-product generated and synthesized by a peptide bond in each step has water solubility and is easily separated, and the liquid-phase synthesis method which has a simple and convenient process and lower cost is provided for the synthesis of the dipeptide diaminobutyroyl benzylamide diacetate.

The invention discloses a preparation method of ultrathin tungsten selenide nanometer slices, and particularly relates to an oil phase method for preparing tungsten selenide. The material has the property of catalyzing benzylamine to produce imine through coupling. The method provided by the invention belongs to the technical field of material preparation and application. A Schlenk line route is used; oleylamine, oleic acid, octadecene and N-dodecyl mercaptan are used as solvents; a selenium source and a tungsten source at a certain ratio are used as reactants for preparation at a certain reaction temperature to obtain the feather-shaped ultrathin nanometer slices with the thickness being smaller than 2nm; the nanometer slices have the effect of efficiently catalyzing the benzylamine to produce N-benzylamine through coupling; in cyclohexane and acetonitrile solvents, the yield of N-benzylamine through benzylamine coupling respectively reaches 95 percent and 96 percent. The catalyst hasthe advantages of great specific surface area and high catalysis efficiency; noble metal is not used; the cost is low. The preparation process is simple; the operation is easy; the use of an organictemplate and surfactant is not needed; the preparation method is suitable for industrial production; the prepared tungsten selenide phase is pure; the specific surface area is large; the repeated utilization performance is high.

A preparing process of lacosamide is disclosed. D-serine is adopted as an initial raw material. The method includes: performing amino protection, performing methylation, condensing with benzylamine under a condition of existence of a carboxyl activator, removing an amino protection group, and performing amidation to obtain the lacosamide. The total yield is higher than 66%. The method is high in yield, simple and convenient to operate, high in product purity and especially suitable for industrial production.

The invention discloses a method for synthesizing upadacitinib intermediate. The method includes performing a ring-forming reaction with 2-pentynoate and N-(methoxymethyl)-N-(trimethylsilylmethyl)benzylamine under a catalyst A to prepare a compound (3), by which the compound (7) or the compound (8) can be obtained in various manners. The method especially the first and the third technical schemes,is high in yield and purity and is high in overall yield. The method is simple in post-treatment and is suitable for industrial large-scale production.

The invention discloses a method for enantioselectively synthetizing (S, S)-8H-6H-pyrrolo [3,4-b] pyridine by using (R)-2-phenylglycinol as a chiral inducing reagent. The method comprises the following steps: by taking (R)-2-phenylglycinol as a raw material, carrying out one-step Michael addition reaction and ester exchange reaction to synthetize a intermediate 2; carrying out condensation on the intermediate 2 and acryloyl chloride to obtain a double-ring intermediate 3; carrying out hydrogenation reduction to obtain an intermediate 4 in high stereoselectivity; reacting the intermediate 4 with benzylamine through one-step amine-ester exchange to obtain an intermediate 5; hydrolyzing the intermediate 5 to obtain an intermediate 6; and carrying out ring closing reaction, reducing, removing protecting group on nitrogen to obtain a final product II. The method has the characteristics of favorable stereoselectivity and high yield, and is simple to operate; compared with the traditional method, for no need of hydrogenating and reducing pyridine ring under high pressure, no need of resolution and the like, the preparation method disclosed by the invention is low in cost, safe and reliable, the yield can achieve 20%-30%; and the method is suitable for industrial production.

The invention discloses a preparation method of amino protection (R)-3-amino piperidine, and the preparation method comprises the following steps: (1) in the presence of a first solvent or absence of a solvent, reacting a compound of formula V with benzylamine to obtain a compound of formula VI; (2) in the presence of a second solvent, performing catalytic hydrogenation of the compound of formula VI to remove benzyl to obtain the amino protection (R)-3-amino piperidine. According to the method, the defects of use of expensive metal catalysts and use of high-pressure hydrogenation and various splitting for synthesis of a chiral amino piperidine ring can be avoided, at the same time, the synthetic route is short, the process is simple, the yield is high, and the method is suitable for industrial mass production.

The invention relates to multi-substituted pyridine, in particular to multi-substituted fluorine-containing pyridine which is obtained by performing the reaction of alkynyl imine and benzylamine for 1 to 30h at 60 to 100 DEG C in an organic solvent in the presence of alkali. Various multi-substituted 3-hydrogen, 3-fluorine and 3-trifluoromethyl pyridine derivatives can be synthesized through a cascade reaction of fluoroalkyl alkynyl imine and methylamine. Substituent groups on pyridine rings can be introduced step by step from a very beginning raw material preparation step, and various compounds with bioactivities synthesized by adopting the method can be used for synthesizing insecticides and antibacterial drugs.

The invention relates to a synthetic method of MACAmide. The method includes following steps: with a fatty acid and benzylamine or m-methoxybenzylamine as reaction raw materials, mixing the raw materials in a dichloromethane solution in which HOAt, EDC.HCl and DIPEA are dissolved; performing a reaction with stirring; washing a reaction product with water; and drying a substance being undissolved in water to obtain the MACAmide. The method is simple in processes and the raw materials are easy to obtain. Operation conditions of the method are easy to control. The reaction product can reach a purity of 95% without purification. The invention provides basis for industrialized synthesis of the MACAmide. In addition, the MACAmide has effects of enhancing male reproductive ability and treating male sexual dysfunction. The invention provides market prospects to application of the MACAmide.

The invention relates to a palladium/carbon nanotube catalyst used for selectively supporting palladium nanoparticles in carbon nanotube chamber or outside the nanotube chamber in alpha, beta unsaturated carboxylic acid hydrogenation reaction, which takes carbon nanotube as a carrier, the palladium nanoparticles can be selectively dispersed in the carbon nanotube chamber or outside the nanotube chamber, the size is uniform, and the particle size is 2-5nm. The catalyst can be used for hydrogenation and asymmetric hydrogenation of asymmetric carboxylic acid. The catalyst appears higher activity than that of the commercialized palladium catalysts in an alpha-phenylcinnamic acid hydrogenation reaction, and the highest reaction activity can reach 564mmol h<-1> g<-1>. When a chiral modification agent cinchonidine and an auxiliary agent benzylamine are added in a reaction system, the enantiomer selectivity of alpha-phenylcinnamic acid asymmetric hydrogenation product can reach more than 75%, the activity is increased to 133mmol h<-1> g<-1>, which is the highest intrinsic reaction activity of a heterogeneous catalyst to the asymmetric hydrogenation reaction of alpha-phenylcinnamic acid.

The invention discloses a cupric ion fluorescence enhancement type molecular probe and a preparation method as well as application thereof. The molecular formula of the probe is shown in the description; 4-methyl-7-hydroxy coumarin is taken as a fluorescence matrix, and reacts with hexamethylene second-amine; a formyl group is introduced at an ortho-position of hydroxy, and an obtained intermediate reacts with o-ethoxyphenol benzylamine; then nitrogen atoms and oxygen atoms are introduced; meanwhile the fluorescent light of a compound is enabled to close, and a specific reaction with cupric ions can be performed. By introducing the nitrogen atoms and the oxygen atoms for performing specific coordination with the cupric ions in the reaction matrix, a cupric ion sensor can quickly cooperate with the cupric ions in a detection process, so that fluorescent light is increased rapidly, thus realizing detection on the cupric ions and being capable of effectively avoiding the disturbance of other metal ions. The fluorescence probe prepared by the method is a high-selectivity fluorescence enhancement type cupric ion chemosensor simple in structure, cheap and easily available in material, easy to prepare and high in yield.

The present invention is the technological process of extracting gibberellic acid GA4+7 from gibberellic acid fermenting liquid. The technological process includes the following steps: regulating the pH value of the filtrate of fermenting liquid to 4.5-4.8 before further filtering through available filter cake to eliminate protein, heavy metal and metal ion; regulating pH value to 6.5-6.8 before concentrating the filtrate by 18-20 times; regulating pH value to 4.2 before extracting with ethyl acetate; centrifuging in a high speed centrifuge, concentrating, diluting with n-butanol, precipitating in N.N-methyl benzylamine, and separating alcohol phase and water phase to obtain GA4+7 of 90 % over purity and GA4/GA7 ratio of 2 to 1. The present invention has high GA4+7 yield and low production cost.