5105 results about "Acylation" patented technology

The invention discloses a preparation method of Roxadustat. The preparation steps are as follows: the Roxadustat is prepared from tyrosine through esterification, etherification, cyclization, dehydrogenation, oxidative rearrangement and acylation reaction. The preparation method has the advantages that the raw materials are easily obtained; the process is simple; and the preparation method is economic and environmental-friendly, and is suitable for industrialized production.

A process for producing a sulfonylpyrrole compound useful as a medicine, a process for producing an intermediate for use in the process, and a novel intermediate. The process for producing a sulfonylpyrrole compound (VIII) comprises reducing a compound (III), subsequently hydrolyzing the compound to obtain a compound (IV), sulfonylating the compound (IV) to obtain a compound (VI), and aminating the compound (VI) to thereby produce the compound (VIII).

The present invention relates to the preparation of a series of oxidized cellulose esters suitable for use as a drug carrier in the development of biodegradable controlled and/or sustained release pharmaceutical, agricultural, and veterinary compositions, such as films, compacts, microspheres, and pellets. The esters are prepared by acylation of oxidized cellulose having at least 3% carboxyl groups. The resulting oxidized cellulose esters are soluble in aqueous alkaline solutions, water, and a variety of organic solvents.

A process for making a surfactant composition involving: (a) providing a starting mixture containing: (i) an aqueous alkali solution; (ii) at least one amino acid and/or a salt thereof; (iii) a fatty acid chloride; (iv) an acylatable surfactant precursor selected from the group consisting of a protein hydrolyzate, a polyamino acid, an aminosulfonic acid, an amino sugar, a nonionic surfactant, and mixtures thereof; and (v) up to about 15% by weight, based on the weight of the starting mixture, of a polyol component; (b) providing a stirring mechanism; and (c) reacting (ii) and (iii), with stirring, to form the surfactant composition.

A process for treating organic compounds includes providing a composition which includes a substantially mesoporous structure of silica containing at least 97% by volume of pores having a pore size ranging from about 15 Å to about 30 Å and having a micropore volume of at least about 0.01 cc/g, wherein the mesoporous structure has incorporated therewith at least about 0.02% by weight of at least one catalytically and/or chemically active heteroatom selected from the group consisting of Al, Ti, V, Cr, Zn, Fe, Sn, Mo, Ga, Ni, Co, In, Zr, Mn, Cu, Mg, Pd, Pt and W, and the catalyst has an X-ray diffraction pattern with one peak at 0.3° to about 3.5° at 2θ. The catalyst is contacted with an organic feed under reaction conditions wherein the treating process is selected from alkylation, acylation, oligomerization, selective oxidation, hydrotreating, isomerization, demetalation, catalytic dewaxing, hydroxylation, hydrogenation, ammoximation, isomerization, dehydrogenation, cracking and adsorption.

An oral dosage form comprises cromolyn sodium (sodium or disodium cromoglycate), and an acylated amino acid delivery agent.

The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

The invention discloses a polymer microsphere and preparation method thereof. The microsphere comprises a core and surface graft; wherein the core is monodispersed polystyrene-divinyl benzene microsphere with crosslinking degree of 60-90% and grain diameter of 2-20 microns, and the surface graft is polyglycidyl methacrylate or derivate thereof. Friedel-Crafts acylation is utilized, alpha-halogenacyllhalide is taken as acylation agent, initiator molecule is bonded on the surface of the microsphere; conventional atom transfer radical polymerization method is utilized to initiate monomers glycidyl methacrylate to condense; then different nucleopilic reagent is utilized for opening ring, and amino, hydroxyl, hydrazine, carboxyl and sulfydryl groups are introduced onto the surface of the microsphere. The polymer microsphere can be used as separation material for different chromatographs for high efficiency ion exchange, chelation and high efficiency affiliation, also can be used as carrier for fixing enzyme and catalyst and is an excellent functional microsphere.

The invention concretely relates to a synthetic technology for pyraclostrobin. The synthetic technology comprises: firstly performing cyclization to obtain 1-(4-chlorophenyl)-pyrazol-3-one, oxidizing the pyrazol ring under the effect of an oxidant to generate 1-(4-chlorophenyl)-3-hydroxypyrazole, then using 2-nitrobenzyl bromide to performing etherification to generate 1-(4-chlorophenyl)-3-[2-(nitrophenyl)methoxy]-1H-pyrazole, then using a reducing agent to perform nitro reducing, so as to generate N-hydroxyl-2-[N'-(4-chlorophenyl)pyrazol-3'-yloxymethyl]aniline, then using ClCO2CH3 to perform N-acylation reaction to generate methyl N-hydroxyl-N-2-{[N'-(4-chlorophenyl)pyrazol-3'-yloxymethyl]phenyl}formate, and finally performing hydroxyl methylation under an alkaline condition to generate pyraclostrobin. The technology enables all operations in the pyraclostrobin preparation process to be relatively controllable, helps to improve the stability of the preparation process and improve the product yield, successfully employs low-cost reagents and substantially reduces production cost, and also the employed reagents are relatively small in toxicity, is relatively beneficial for environment protection, and has no corrosivity on plastic pipes, so that the production safety is improved.

The invention discloses a synthetic method for loxoprofen sodium, which is prepared by taking methyl acetophenone as an initial raw material through reduction, acylation or halogen substituent, cyanation, hydrolysis, bromination, condensation, decarboxylation and salifying. The method has the advantages of easily obtained raw material, unique technology, simple and stable operation, and high productive rate in each step of reaction; and all solvents used in the synthesis process can be recycled, so the production cost is reduced greatly. Tests show that the obtained product has reliable quality and stable performance, and can be further used for making preparation of non-steroidal anti-inflammatory drugs such as the loxoprofen sodium.

The present invention relates to a composition for treating skin comprising an acylated short chain bioactive peptide and fulvic acid, and optionally colloidal gold. The invention further relates to a method for topically administering the composition in an amount therapeutically effective to reduce wrinkles by building the dermal fibroblast matrix. The invention further relates to a method of treating wrinkled skin by topically administering the composition to an individual in need of such treatment.

A preparation method of a carbon fiber reinforcement grafted by graphene oxide relates to a preparation method of a carbon fiber reinforcement grafted by graphene oxide. The invention solves the problems of harsh process conditions, long process period, toxic process, and difficult industrial production for current carbon fiber surface modification methods. The invention adopts a 'grafting' method, and grafts graphene oxide on acidified carbon fiber surfaces through an acylation reaction by using polyamide-amine with a lot of amido active groups; the invention has low cost, is simple, practical, environment-friendly, and nontoxic, and can be completed within a short period. The method particularly comprises the following steps: mixing acidified carbon fibers and a polyamide-amine methanolsolution, reacting to prepare carbon fibers modified by polyamide-amine, adding the prepared carbon fibers in a graphene oxide acetone suspension, mixing, reacting, filtering, drying the precipitatestill the weight is constant. The obtained carbon fiber reinforcement has interfacial shear strength with epoxy resin of up to 79.77-105.50 MPa which is improved.

The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative.

This invention provides an easy and efficient process for producing a simvastatin of great use as an HMG-CoA reductase inhibitor, which comprises deacylation of lovastatin with an inorganic base and a secondary or tertiary alcohol and subjecting the resulting diol lactone to selective protection with a ketal or acetal protective group, acylation and deprotection-lactonization to give simvastatin.

The invention discloses a mesosulfuron-methyl synthetic method. The mesosulfuron-methyl synthetic method is characterized in that mesosulfuron-methyl is prepared from raw materials such as paratoluic acid by adopting the seven steps of chlorosulfonation-ammonolysis, oxidation, dehydration, reduction, alcoholysis, methyl sulfone chloride acylation and condensation. The mesosulfuron-methyl synthetic method provided by the invention has the advantages of being low in cost of the raw materials, easy in availability of the raw materials, simple in operation and mild in conditions, having low requirements on equipment, high yield and strong practicability and being suitable for industrial production.

The invention discloses a synthetic process for efficiently and continuously producing 4,4-dichlorodiphenyl sulfone, which comprises the following steps: carrying out Friedel-Crafts acylation on thionyl chloride and excessive chlorobenzene under the action of a lewis acid catalyst, carrying out pyrohydrolysis and adding chlorobenzene to carry out layering after the reaction is finished, adding anoxidizing agent into a sulfoxide organic layer to carry out oxidization, adding activated carbon to carry out decoloration and filtering; cooling filtrate and carrying out rejection filtration to obtain 4,4-dichlorodiphenyl sulfone. The synthetic process has the advantage that chlorobenzene not only is a raw material, but also is a reaction solvent, so that cross use of various solvents is avoided. Particularly, use of a great amount of acetic acid used as an oxidation reaction solvent is avoided, and corrosion to equipment and environmental pollution are avoided. In the integral process flow,separation and extraction of an intermediate 4,4-dichlorodiphenyl sulfoxide are avoided, so that production time of the product is greatly shortened, and production cost is saved. By using hydrogen peroxide, acetic acid and concentrated sulfuric acid as mixed oxidizing agents, oxidization capacity of hydrogen peroxide is greatly improved, yield and purity of the product are greatly improved, yield of the product reaches 90% or more, and purity of the product is greater than 99.8%.

The invention aims at acid, alkali and heat labile features of sinomenine molecular structure, and provides an innovative structural reconstruction idea for new chemical synthesis of ring A, ring C, and ring D sinomenine derivatives. The chemical synthetic method includes amination and acylation of 1-position, C-C or C-O connection of 1 position, dicarbonylation and six-membered N heterocyclization of 3-position and 4-position, two molecule sinomenine adduction of connection of 4-hydroxyl and 1-amino, amination and acylation of 6-position, simultaneous amination and x-membered N heterocyclization of 6-position and 7-position, and opening of D ring and terminal amino group modification thereof. The method is novel and unique. The sinomenine derivatives have good antiinflammation activity and bioactivity evaluated by synovial membrane tumor cell (SW982), and can be used in drug and health products for resisting rheumatoid arthritis.