604 results about "Amino Acylation" patented technology

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 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.

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.

The invention discloses thermosensitive hydrogel loaded with copper metal organic skeleton nanoparticles and a preparation method of the thermosensitive hydrogel. The preparation method comprises thesteps that an amino group on gelatin and methacrylic anhydride are subjected to acylation reaction to synthesize methylacrylic esterified gelatin with a branch containing a carbon-carbon double bond,the carbon-carbon double bond on the branch and N-isopropyl acrylamide are subjected to free radical polymerization, and methylacrylic esterified gelatin-g-poly N-isopropyl acrylamide is prepared; 1,3,5-benzene tricarbonic acid and copper acetate monohydrate are used for preparing copper-based MOF nanoparticles; the copper-based MOF nanoparticles are added to a methylacrylic esterified gelatin-g-poly N-isopropyl acrylamide solution, and a product is prepared. Copper ions are embedded in the biodegradable thermosensitive hydrogel in the form of HKUST-1 NPs, controlled slow release of the copperions is achieved, cytotoxicity is effectively reduced, migration of in-vitro dermal cells is promoted, angiogenesis is induced, and wound healing is promoted.

The invention discloses a CPC acylation enzyme whose encode gene is DNA sequence shown as SEQ IN NO: 4 and DNA sequence having at least 80154000mology with the above DNA sequence. The invention also discloses carriers and transformants containing coding CPC acylation enzyme and the use of the enzyme. The enzyme has high expressing activity, high catalytic activity and high outcome tolerance to catalysis bottom object in high efficiency to prepare outcome 7-ACA.

Method of performing condensation reactions, acylations or of preparing heterocycles comprising forming cyclic phosphonic anhydride of the formula (III) by a) reacting phosphonic acid derivatives of formula (I) with acetic anhydride at a temperature ranging between 30 and 150° C. while separating a mixture of ethanoic acid and acetic anhydride by means of distillation, b) then reactively distilling the oligomeric phosphonic acid anhydrides of formula (II) obtained in step a) and transforming the same into the corresponding cyclic trimeric phosphonic acid anhydrides of formula (III), wherein n represents a number between 0 and 300 while R represents allyl, aryl, or open-chain, cyclic, or branched C1 to C8 alkyl radicals, aryloxy, allyloxy, or alkoxy comprising open-chain, cyclic, or branched C1 to C8 alkyl radicals. Preferably the cyclic trimeric phosphonic acid anhydrides formed in step b) are immediately dissolved in an organic solvent that exhibits an inert behavior relative thereto.

The invention discloses a method for on-line synthesizing sucrose-6-acetate catalyzed by lipase. According to the method, sucrose and vinyl acetate with a molar ratio being 1 : 15-20 are used as raw materials; 0.5-1.0 g of the lipase (Lipozyme TLIM) is used as a catalyst and a mixed solvent formed by tert-amyl alcohol and DMSO is used as a reaction solvent. The lipase (Lipozyme TLIM) is uniformly filled in a reaction channel of a microfluidic channel reactor, wherein the inner diameter of the reaction channel of the microfluidic channel reactor is 0.8-2.4 mm, and the length of the reaction channel is 0.5-1.0 m; the raw materials and the reaction solvent are continuously introduced into the reaction channel for an acylation reaction, wherein the temperature of the acylation reaction is controlled at 40-55 DEG C and the time of the acylation reaction is 20-40 min; a reaction liquid is collected on-line; and the sucrose-6-acetate is obtained after the reaction liquid is subjected to conventional post-treatment. The method provided by the invention has the advantages of short reaction time, high selectivity and high yield.

The invention relates to a method for preparing Decitabine. The particular proposal for solving the technical problem is as follows: 2-deoxidtion-D-ribose, 10 percent of HCL methanol solution, methoxyacetic acetic anhydride, HMDS, acetic anhydride, tri-silicyl tri-fluorine methane sulfonic acid ester, acetic acid amine, etc. are adopted as raw materials to synthesize the Decitabine; the target product of the Decitabine is obtained through the five steps of reactions, namely, methylation, acylation, trimethyl silication, ammoniation and deacylation with a total yield of above 18.4 percent and a product purity of above 99.7 percent.

The invention discloses a synthesis process of 2-amino-4-acetamino anisole. The synthesis process comprises the following steps: in methanol, under the action of an acid-binding agent, 2,4-diaminoanisole (III) and acetic anhydride are subject to acylation reaction shown in the description to obtain 2-amino-4-acetamino anisole (IV), wherein the molar ratio of the acid-binding agent to 2,4-diaminoanisole is (0.3 : 1)-(0.6 : 1). The synthesis process is low in energy consumption and cost, less in waste solids and waste liquid, environment-friendly, simple in operation, mild in reaction condition and high in industrial safety factor, the yield of the target compound is above 86% (counting according to original reaction raw materials), the HPLC purity is above 99.0%, the target compound is high in yield and good in quality, and the synthesis process is more suitable for industrial production.

A process for producing esters of citric acid from citric acid and linear or branched aliphatic monoalcohols of 4 to 14 carbon atoms wherein the essential characteristics are the use of a limited stoichiometric excess amount of alcohol relative to the acid employed and the immediate acylation of the unprocessed ester, i.e. the conversion of the unprocessed ester with an acylating agent for masking the OH- group without having previously subjected it to any purification operation.

The invention discloses a method of using lipase to catalyze and synthesize glucose-6-laurate on line. The method comprises the following steps: taking glucose and vinyl laurate as raw materials according to molar ratio of 1:8-12, taking 0.5-1.0 g of lipase Lipozyme TLIM as a catalyst, taking tert-amyl alcohol and DMSO (dimethyl sulfoxide) mixed solvent as a reaction solvent, uniformly filling the lipase Lipozyme TLIM into a reaction channel of a microfluidic channel reactor, wherein the inner diameter of the reaction channel of the microfluidic channel reactor is 0.8-2.4 mm, and the reaction channel is 0.5-1.0 m long, continuously introducing the raw materials and the reaction solvent into the reaction channel to perform acylation reaction, controlling the temperature of acylation reaction to be 40-55 DEG C, and keeping the acylation reaction for 15-35 min, on line collecting reaction liquid, and conventionally post-processing the reaction liquid to obtain glucose-6-laurate. The method has the advantages of short reaction time, high selectivity and high yield.

The subject invention lies in the field of vaccines. Specifically new compounds that can be used as adjuvants are provided. Recombinant LPS having a reduced number of secondary acyl chains per molecule of LPS vis a vis the corresponding non modified LPS molecule, said secondary acyl chains being bound to primary acyl chains, said primary acyl chains being bound to the glucosamine of said recombinant LPS molecule, said recombinant LPS being homogenous in acylation pattern is an example of such a compound. Also recombinant LPS having a phosphate group attached to the glucosamine at the non reducing end of the LPS molecule and a phosphate group attached to the glucosamine at the reducing end of the molecule per recombinant LPS molecule provides a further example.

The invention relates to a 2-(2'-hydroxyphenyl) benzothiazole chelated zinc derivative as well as a preparation method and an application thereof, belonging to the field of organic electroluminescentluminescent materials. The preparation method of the derivative comprises the following steps: firstly, introducing different substituent groups with electron-withdrawing or electron-donating capability in a benzothiazole benzene ring or a hydroxyphenyl benzene ring of a 2-(2'-hydroxyphenyl) benzothiazole matrix to obtain a substituted 2-(2'-hydroxyphenyl) benzothiazole ligand; coordinating with diatomic zinc to form a corresponding complex, and the like. The substituted 2-(2'-hydroxyphenyl) benzothiazole ligand can be prepared by a plurality of reactions, such as substituted aniline acylation, hydroxyl protection, hydroxyl thiocarbonate, Jacobson cyclization while hydroxyl deprotection, and the like or prepared by a direct reaction of O-amino thiophenol and substituted ortho-hydroxybenzoic acid. When applied to an organic electroluminescent luminescent device as an electronic transmission layer, the derivative has favorable electronic transmission performance and has performance superior to the most common electronic transmission material 8-hydroxyquinoline aluminum.

The invention relates to the application of a gene engineering technology in increasing an antibiotic component, in particular to a gene series technology for increasing the main component content ofgene engineering isovaleryl selectomycin. The gene series technology comprises the following steps: connecting ist genes which are closely related to selectomycin isovaleryl acylation in Beta selectomycin gene engineering bacteria in series; increasing the bacterial isovaleryl acylation generating capability by increasing gene dosage; using a promoter erythrocin resistance gene erm promoter sequence with strong promotion activity to replace the original ist gene promoter sequence so as to increase the expression of the series ist genes, and improve the proportion of isovaleryl selectomycin main components of the gene engineering bacteria from a headstream.

Described herein are methods for producing recombinant forms of asparaginase derived from Wolinella succinogenes. In addition, methods for covalent modification of proteins, including asparaginases, by acylation are also provided. Certain embodiments provide for epitopic-labeling of the amino terminus of W. succinogenes asparaginase. Additional embodiments concern methods for the therapeutic utilization of the native, homotetrameric form of W. succinogenes asparaginase, as well as the use of epitopically-labeled or non-epitopically-labeled recombinant W. succinogenes asparaginase (or a covalently modified analog thereof) in the therapeutic treatment of malignant and non-malignant hematological disease and other diseases where asparagine depletion or deprivation would be efficacious or which respond to asparagine depletion or deprivation, as well as their potential utilization in the therapeutic treatment of autoimmune diseases such as rheumatoid arthritis, AIDS, and SLE.

The invention discloses a mesoporous titanium dioxide immobilized enzyme, which comprises enzyme and a carrier to immobilize the enzyme. The enzyme is a gamma- glutamyltranspeptidase, and the carrier is mesoporous titanium dioxide. The invention also discloses a preparation method of the mesoporous titanium dioxide immobilized enzyme and application thereof. The mesoporous titanium dioxide immobilized enzyme obtained through the invention has the advantages of homogeneous property, large surface area, high enzyme stability, good reusability and the like, and establishes foundations to further improve the stability of the gamma-glutamyltranspeptidase and expand the industrial application of the glutamyl acylation reaction.

The invention provides a chemical method for preparing 5,6,4'-trihydroxyflavone-7-O-D-glucuronic acid to solve problems of unavailable raw materials, long synthetic route and low synthesis yield in the existing synthetic method. The method comprises a plurality of chemical reaction steps: first, taking 3,4,5-trimethoxy phenol and p-methoxy cinnamoyl chloride as the raw materials to construct a chalcone structure by a Friedel-Crafts acylation reaction, and cycloetherifying to obtain a flavone parent substance; then protecting and selectively deprotecting phenolic hydroxyl of the flavone parent substance, and glycosylating 7-phenolic hydroxyl; and finally removing a protective group to obtain the target compound. The obtained product has a beta-steric configuration. The method can be used for preparing high-purity and high-quality 5,6,4'-trihydroxyflavone-7-O-D-glucuronic acid products.

The invention provides four triptolide derivatives and a preparation method of corresponding agents, which uses triptolide as raw material, via acylation and nucleophilic substitution to obtain triptolide derivative to be reacted with acid or alkyl halide to obtain a corresponding salt which can be added with one or more pharmaceutically acceptable adjuvants to prepare relative agent-freeze-driedpowder.

The invention discloses a method for synthesizing laurel acyl amino acid sodium. The method comprises the steps that lauric acid and phosgene react by being catalyzed by organic aryl amide, and lauroyl chloride is prepared; lauroyl chloride and amino acid react in an alkaline solution, and lauroyl amino acid salt is prepared; extraction separation is carried out, a catalyst is recycled from an organic phase, a water phase is sequentially subjected to acidification, filter separation, sodium hydroxide neutralizing and cooling crystallization, and laurel acyl amino acid sodium is obtained. According to the method, organic aryl amide is mainly adopted as the catalyst for the reaction of lauric acid and phosgene, the lauric acid acylation reaction is thorough, no residue exists, acyl chloride products do not need layering, distilling and other purifying processes can be directly used for synthesizing laurel acyl amino acid sodium, and especially the catalyst can be recycled and cyclically utilized through a simple method. Compared with use of existing DMF and other fatty amine catalysts, the process steps are greatly simplified, the yield and quality of the product are improved, production cost is reduced, environmental protection is facilitated, and the requirements of industrial production are met.

The invention discloses a preparation method of a new drug acalabrutinib applicable to treatment of leukemia. The preparation method comprises the steps of condensation, acylation, cyclization, amination and other reactions by using 3-chloro-2-formylpyrazine as the raw material, thereby obtaining the acalabrutinib. The preparation method of acalabrutinib has the advantages of accessible raw materials, simple technique and the like, is economical and environment-friendly, and is suitable for large-scale industrial production.

The invention discloses a method of using lipase to catalyze and synthesize mannose-6-laurate on line. The method comprises the following steps: taking mannose and vinyl laurate as raw materials according to molar ratio of 1:8-12, taking 0.5-1.0 g of lipase Lipozyme TLIM as a catalyst, taking tert-amyl alcohol and DMSO (dimethyl sulfoxide) mixed solvent as a reaction solvent, uniformly filling the lipase Lipozyme TLIM into a reaction channel of a microfluidic channel reactor, wherein the inner diameter of the reaction channel of the microfluidic channel reactor is 0.8-2.4 mm, and the reaction channel is 0.5-1.0 m long, continuously introducing the raw materials and the reaction solvent into the reaction channel to perform acylation reaction, controlling the temperature of acylation reaction to be 40-55 DEG C, and keeping the acylation reaction for 15-35 min, on line collecting reaction liquid, and conventionally post-processing the reaction liquid to obtain mannose-6-laurate. The method has the advantages of short reaction time, high selectivity and high yield.

The invention discloses a method for on-line synthesizing glucose-6-acetate catalyzed by lipase. According to the method, glucose and vinyl acetate with a molar ratio being 1 : 16-22 are used as raw materials; 0.5-1.0 g of the lipase (Lipozyme TLIM) is used as a catalyst and a mixed solvent formed by tert-amyl alcohol and DMSO is used as a reaction solvent. The lipase (Lipozyme TLIM) is uniformly filled in a reaction channel of a microfluidic channel reactor, wherein the inner diameter of the reaction channel of the microfluidic channel reactor is 0.8-2.4 mm, and the length of the reaction channel is 0.5-1.0 m; the raw materials and the reaction solvent are continuously introduced into the reaction channel for an acylation reaction, wherein the temperature of the acylation reaction is controlled at 40-55 DEG C and the time of the acylation reaction is 15-35 min; a reaction liquid is collected on-line; and the glucose-6-acetate is obtained after the reaction liquid is subjected to conventional post-treatment. The method provided by the invention has the advantages of short reaction time, high selectivity and high yield.

The invention relates to water-soluble near infrared luminescent quinoline squaraine dye, of which the molecular structural general formula is shown on the figure. The method for preparing the water-soluble near infrared luminescent quinoline squaraine dye comprises that: firstly, 2-methylquinoline is subjected to bromination, sulfonation, nitration and acylation and reacts with acetonitrile and iodo-acid or iodo-ester to generate quinoline quaternary ammonium salt; and secondly, the quinoline quaternary ammonium salt is mixed with squaric acid, and the mixture is subjected to azeotropic distillation and dehydration, vacuum distillation and silica gel column chromatography and recrystallization through ethanol to obtain the water-soluble quinoline squaraine dye. The dye is applied in the fields of development of novel medicines, fluorescence labeling, probes, biological immunoassay, biological immunodetection and the like. The fluorescence-emission wavelength of the water-soluble quinoline squaraine dye is near infrared, so that the water-soluble quinoline squaraine dye has superior penetrability on environments and biological tissues and reduces self absorption and background absorption, and the sensitivity of fluorescence analysis can reach 10<-10> mol / L. The preparation method is simple and easy, has low cost and good economic benefit and is suitable for industrialized production.

The invention discloses a room temperature phosphorescent compound and a preparation method, a single crystal culture method and application thereof in the field of anti-counterfeit. According to the invention, through acylation reaction with the participation of aluminum trichloride or sodium hydride, benzoyl chloride and derivatives thereof react with carbazole, benzoyl or derivatives thereof are connected with carbazole through N atoms, and by changing R groups connected with the benzoyl, three room temperature phosphorescent compounds CPM (R=H), CMPM (R=CH3) and CMOPM (R=OCH3) are obtained, and then the three compounds are cultured into single crystals through a solvent volatilization method by using two solvents with different solubility, boiling point and volatility. The obtained single crystals can be used in the field of anti-counterfeit, and can be matched with a material with better fluorescence-emission ability in use to complete two modes: color reliquid and time reliquid. Especially, the phosphorescence life of the obtained compound CPM at room temperature reaches 748ms, so that the compound CPM can be practically used in the field of anti-counterfeit.

The invention discloses self-repairing and photo-sensitive chitosan hydrogel and a preparation method thereof. The preparation method of the chitosan hydrogel comprises the steps as follows: (1) carboxymethyl chitosan and nitro-dopamine are taken as raw materials and subjected to acylation reaction, and a chitosan derivative containing a nitro-dopamine group is obtained; (2) a chitosan derivative aqueous solution containing the nitro-dopamine group is mixed with a Fe <3+> solution, the pH of the mixed solution is adjusted to 6.5-9.5, and the self-repairing and photo-sensitive chitosan hydrogel is obtained. The chitosan derivative containing the nitro-dopamine group and a metal ion are coordinated to be crosslinked with a mussel bionic chemistry method, and dopamine has good biocompatibility, so that toxicity to organisms due to hydrogel prepared with a traditional method is reduced; the prepared self-repairing and photo-sensitive chitosan hydrogel has high adhesion, good compliance and high time and space controllability, and can maintain the best moist environment for a long time on the wound surface, promote wound epithelialization and accelerate wound healing when used as a wound dressing.

The invention discloses a process for preparing Quinclorac artificial semiantigen, artificial antigen, specific antibody and use thereof, wherein the preparation comprises, subjecting the dichloroquine (3,7-dichlorine-8-quinoline carboxylic acid) to sulfoxide chlorinated acylation, reacting with reanal and aminocaproic acid, thus obtaining semiantigen 4-(3,7-dichlorine-8-quinolineformyl) reanal or 6-(3,7-dichlorine-8-quinolineformyl) aminocaproic acid (QB or QC).

Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide.Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.

The invention discloses a preparation method of a ferrocenyl carbon nanotube composite material and application thereof and belongs to the technical field of synthesis of inorganic materials. The preparation method of the composite material comprises the following steps: firstly carrying out oxidization and amination on carbon nanotubes and carrying out acylation on ferrocenecarboxylic acid, then taking triethylamine as an acid-binding agent in a dichloromethane solvent, and enabling the carbon nanotubes subjected to amination to react with activated ferrocenylformyl chloride to prepare the composite material. The preparation method of the composit material is simple and is mild in reaction condition; the product is convenient to separate and purify and stable in structure. The composite material takes the carbon nanotubes with large specific surface area and high conductivity as support materials; ferrocenyl derivatives which can be used as electron media and provided with excellent electrochemical reversibility are covalently coupled on the surfaces of the carbon nanotubes, so that the composite material is excellent in effect of redox reaction for electrochemically catalyzing dopamine; the common interference matters including ascorbic acid and uric acid have no interference on detection of dopamine; the composite material is wide in linear response range and high in sensitivity and repeatability for detection of dopamine.