190 results about "Acylal" patented technology

The present invention is directed to conjugates such as polymeric prodrugs of aromatic, hydroxyl-containing compounds and methods of making and using the same. These polymeric prodrugs are preferably esters of hydroxyl-containing aromatic compounds and are formed by reacting a desired aromatic, hydroxyl-containing compound with a substantially non-antigenic polymer so as to produce a transport form having an ester linkage between the aromatic compound and the polymer. Preferred aromatic hydroxyl-containing compositions include 10- and 11-hydroxycamptothecin derivatives. Methods of treatment are also disclosed.

A cellulose acylate which is a polymer obtained by substituting cellulose with acyl groups in 2-, 3-, 6-positions. The total degree of acyl substitution in the 2- and 3-positions is regulated to from 1.70 to 1.90. The degree of 6-position acyl substitution is regulated to 0.88 or higher.

The present invention provides a cellulose ester composition, containing 1 to 99% by weight of cellulose triacetate prepared by substituting hydroxyl groups of cellulose with acetyl and having a degree of substitution with acetyl, DSace, which satisfies the relationship: 2.7< / =DSace< / =3.0, and 99 to 1% by weight of a mixed fatty acid ester of cellulose prepared by substituting hydroxyl groups of cellulose with acetyl and acyl groups having three or more carbon atoms and having degrees of substitution with acetyl and acyl groups having three or more carbon atoms, DSace and DSacyl, respectively, which satisfy the relationships: (I) 2.20< / =DSace< / =2.95, (II) 0.05< / =DSacyl< / =0.80 and (III) 2.60< / =DSace+DSacyl< / =3.00.

The present invention relates to novel 2-carbonyl-3-acyl-1,3-thiazolidines having a β-amino group on the acyl chain, in free, prodrug form or pharmaceutically acceptable salt thereof, including their enantiomers, diastereomers and racemates, as efficient inhibitors against DPP-IV. The invention further relates to the pharmaceutical compositions comprising the disclosed compounds. The present invention also relates to methods for preparing the disclosed compounds and for treating DPP-IV-mediated diseases.

Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.

The present invention provides glycoconjugates that are formed through the enzymatically-mediated coupling of a glycosyl moiety, e.g., on a peptide or lipid, and a modifying group that includes an acyl group. The conjugates include the modifying group tethered to the glycosyl moiety through a linking moiety that includes an acyl residue. Also provided are methods for preparing the conjugates of the invention

The invention relates to comb polymers which comprise, in the main chain, repeating units which are derived from polyolefin-based macromonomers, and repeating units which are derived from low molecular monomers which are selected from the group consisting of styrene monomers having 8 - 17 carbon atoms, alkyl(meth)acrylates having 1 - 10 carbon atoms in the alcohol group, vinyl esters having 1 - 11 carbon atoms in the acyl group, vinyl ethers having 1 - 10 carbon atoms in the alcohol group, (Di)alkylfumarates having 1 - 10 carbon atoms in the alcohol group, (Di)alkylmaleates having 1 - 10 carbon atoms in the alcohol group and mixtures of said monomers. The molar branching degree lies in the region between 0.1 - 10 mol. % and the comb polymer represents the sum of at least 80 wt. %, in relation to the weight of the repeating units, on repeating units which are derived from polyolefin-based macromonomers, and repeating units which are selected from low molecular monomers which are selected from the group consisting of styrene monomers having 8 - 17 carbon atoms, alkyl(meth)acrylates having 1 - 10 carbon atoms in the alcohol group, vinyl esters having 1 - 11 carbon atoms in the acyl group, vinyl ethers having 1 - 10 carbon atoms in the alcohol group, (Di)alkylfumarates having 1 - 10 carbon atoms in the alcohol group, (Di)alkylmaleates having 1 - 10 carbon atoms in the alcohol group, and mixtures of said monomers.

A cellulose acylate which is a polymer obtained by substituting cellulose with acyl groups in 2-, 3-, 6-positions. The total degree of acyl substitution in the 2- and 3-positions is regulated to from 1.70 to 1.90. The degree of 6-position acyl substitution is regulated to 0.88 or higher.

A method for producing a diacylglycerol-rich fat or oil is provided. This method includes the steps of reacting an acyl group donor with an acyl group receptor, and separating unreacted material and byproducts by distillation for use as a part of the starting material in the subsequent cycle of production. The distillation is conducted such that the content of monoacylglycerol in the fat or oil after the distillation is 0.5 to 15% by weight.

A thiophene compound represented by formula (I): in which A represents a C1-5-alkylene bridge; R represents a —R1—(C═O)—R2 group; —R1— represents a —R3— or —R4—X—R5— group; R2 is hydrogen, a hydroxy group, a thiol group, —NR6R7, —OR8 or a —SR9 group; R3, R4 and R5 are independently an alkylene group or an arylene group; X is a —O—, —S— or ═NR10; R6 and R7 are independently hydrogen, an optionally substituted amino group or an optionally substituted alkyl group; R8 and R9 are independently an optionally substituted alkyl group (optionally with at least one substituent selected from the group consisting of an alcohol, amide, ether, ester or sulfonate group), an optionally substituted aryl group or a —SiR11R12R13 group; R10 is an alkyl, aryl or acyl group; and R11, R12 and R13 are independently an optionally substituted alkoxy or alkyl group; polymers derived therefrom; a process for polymerizing a thiophene according to formula (I), optionally chemically or electrochemically; and solutions, dispersions, pastes and layers containing polymers derived therefrom.

The present invention relates to a starch ester having short- and long-chain acyl groups wherein hydrogens in reactive hydroxyl groups in the same starch molecule have been replaced by C2-4 short-chain acyl groups and C6-18 long-chain acyl groups. The degree of substitution by the short- and long-chain acyl groups are regulated so as to make the starch ester thermo-plasticized and moldable even in the absence of a plasticizer. Accordingly, the starch ester of the present invention can be used as a biodegradable thermoplastic plastic material which can be thermo-plasticized in the absence of a plasticizer.

The invention provides an alkylation preparation method for aniline intermediate, which comprises the following steps: beating the aniline intermediate expressed by formula (1) in aqueous solution, adding an acid-catching agent, a catalyst and an alkylation reagent into the solution, heating the mixture to between 60 and 105 DEG C by stirring, reacting the mixture for 5 to 18 hours through heat preservation, cooling and crystallizing the reaction solution after the reaction is finished, stirring and filtering the solution, taking a filter cake out, and washing and drying the filter cake to obtain an aniline alkylation product expressed by formula (2). The method has the main following advantages that: (1) quaternary ammonium salt and dispersant used as a mixed catalyst in the method have obvious effect of promoting the reaction, can prevent oil-water demixing, can balance the system after the reaction is finished, and are easy to crystallize; and (2) by adopting the acid-catching agent provided by the method, the pH value can be well controlled and stabilized, the hydrolysis of acyl and halogenated hydrocarbon can be effectively prevented, and the occurrence of side reaction and the consumption of the halogenated hydrocarbon can be reduced; and the cost can be reduced and the cost performance can be improved by using heavy magnesium oxide as the acid-catching agent in particular.

The present invention discloses a nucleophilic acyl substitution-based polymerization catalyzed by oxometalic complexes. In the first place, the first monomers with a plurality of carboxyl groups, and the second monomers with a plurality of protic nucleophilic groups are provided, wherein the protic nucleophilic groups comprise hydroxyl, amine, or thiol group. Next, catalyzed by the mentioned oxometallic complex, the first monomers and the second monomers are polymerized into the designed polymer. On the other hand, this invention discloses another nucleophilic acyl substitution-based polymerization catalyzed by oxometallic complexes. In the first place, monomers with at least one carboxyl (phosphonyl) group and at least one masked protic nucleophilic group are provided. Then, monomers are polymerized into the designed polymer, catalyzed by the mentioned oxometallic complexes.

The present invention relates to a plasticizer for biodegradable resin, which contains a compound represented by the following formula (1): wherein at least one of R 1 , R 2 and R 3 is an acyl group derived from a carboxylic acid selected from an aliphatic hydroxycarboxylic acid and an acetylated aliphatic hydroxycarboxylic acid, and the remainder(s) is an acetyl group, a biodegradable resin composition containing biodegradable resin and the plasticizer.

Anhydrous cosmetic antiperspirant stick compositions containing a continuous phase of a water-immiscible cosmetic oil structured by a fibre-forming amido structurant can exhibit undesirable sensory properties when 12-hydroxy-stearic acid is employed as primary gellant and the preparation of sick compositions suffers from sever processing difficulties when certain of such amido structurants are employed as primary gellant. Stick compositions having desirable sensory properties can be made by employing as primary gellant, a combination of amido structurants comprising (i) an N-acylaminoacid amide in which the N-acyl substituent has the formula -CO-R<X >in which R<X >represents a branched C6 to C11 alkyl group and (ii) an N-acylaminoacid amide in which the N-acyl substituent contains a linear alkyl group and the cosmetic carrier oil comprising from 25 to 50% by weight of a water-immiscible monohydric alcohol that is liquid at 20° C. and a boiling point of higher than 100° C.

The present invention relates to a method of preparing optically active amines and chiral amines prepared thereby. The method includes reacting an amine compound, a metal catalyst, a biocatalyst including a lipase, and an acyl donor compound in an organic solvent to obtain a chiral amide compound, and then hydrolyzing the chiral amide compound to obtain a chiral amine.

The present invention relates to a process for making indenol esters or ethers from an α-substituted cinnamic aldehyde derivative such as an acetal or an acylal. Said reaction is promoted by the use of strong mineral acids, sulphonic acids, acidic zeolites or Lewis acids.

Compounds of formula (I)wherein: one of R1, R2, R3, R4 and (R10)n represents halogen and each remaining R1, R2, R3, R4 and R10 group is independently selected from hydrogen, halogen, amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamidosulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl, and corresponding substituted groups; m=0-1; n=1-4, A is nil, O, or NH; R9 is alkylene; -Z is H, amino, dialkylamino, or a trialkylamino salt; X− is an anion; R5, R6, R7 and R8 are independently H or C1-C6 alkyl or R1 in combination with R5 or R6, or R2 in combination with R5 or R6, or R3 in combination with R7 or R8, or R4 in combination with R7 or R8 represents alkylene, are useful alone or with a pharmaceutically acceptable carrier, as intermediates and as bactericides, antiviral agents and in treatment of immunologic disorders.

The invention discloses acyl-substituted triptycene and a preparation method thereof. An acyl compound is represented as structural general formula I or II. A framework of the compound is triptycene with a rigid three-dimensional structure. Two or three acyls are selectively introduced on the triptycene framework and can conveniently polymerized into a polymer through McMurry reaction, and the structure of the produced polymer is represented as general formula VI or VII. The preparation method of the acyl-triptycene derivative has the advantages of being cheap in raw materials, simple in synthetization, high in productivity, easy to derivatize and the like. In addition, the produced polymer has good dissolubility, and the acyl-substituted triptycene can be processed conveniently and has wide application prospect.

The invention provides a method for synthesizing (E)-(2-(phenylsulfonyl)vinyl)benzene and a derivative thereof. The method adopts styrene or a derivative of styrene as a reactant A and sodium benzenesulfinate or a derivative of sodium benzenesulfinate as a reactant B, and the reactant A and the reactant B react under the oxidation of persulphate to generate (E)-(2-(acyl)vinyl)benzene and the derivative thereof. Compared with the conventional method utilizing thioether oxidation, sulfur dioxide addition, Friedel-Crafts sulfonylation and transition metal catalysis coupling, the method increasesyield, and since the method utilizes relatively cheap persulphate as oxidant to carry out reaction, the cost of synthesis is reduced.

A novel cellulose acylate film is disclosed. The film is formed of a composition comprising at least one cellulose acylate having an aromatic group-containing acyl group (Substituent A), in which a substitution degree with Substituent A satisfies following relational expressions (I) and (II):−0.25≦SA2+DSA3−DSA6≦0.20,   (I)0.35≦DSA2+DSA3+DSA6,   (II)wherein DSA2, DSA3 and DSA6 each indicate a substitution degree with Substituent A at the 2-, 3- and 6-positions of the cellulose acylate.

The present invention provides 3-substituted amino-1, 2, 4-substituted phentriazine-1, 4-dioxides in the general expression as shown. The compounds are prepared with substituted one-nitroaniline as main material and through acylation to produce urea, cyclization, chlorination, amino substitution, oxidation and other steps. The tests show that the compounds of the present invention have anticancer activity and hypoxia selectivity higher than those of TPZ and may be used in preparing hypoxia selective anticancer medicine.

The invention discloses a polyether amine and a preparation method thereof, and belongs to the technical field of high polymer material synthesis and preparation. According to the polyether amine and the preparation method thereof, a ketone, an aldehyde or an acid anhydride is reacted with primary amine for the first time to generate ketimine, aldimine or acyl protected amine compounds, and secondary amine or active hydroxyl and an alkylene oxide monomer are subjected to anionic polymerization so as to successfully synthesize polyether amine containing primary amine. The defects that the conventional method, namely, direct hydroxyl amination, requires harsh conditions of the equipment and the process, and side reaction is likely to happen when the amine compound is bonded with a polyether chain, are overcome, and polyether amine which is moderate in reaction condition and tidy in structure is successfully synthesized. The polyether amine has potential application in the fields of machine manufacturing, electrical equipment and electronic devices, communication and transportation, petrochemical engineering, national defense construction, electrophoretic paint, anticorrosive paint and the like.

The invention belongs to the fields of biological catalysis and biotransformation and discloses a method for preparing an esterified derivative of lily polysaccharide by biological catalysis. The method comprises the following steps of catalyzing lily polysaccharide by utilizing lipase for transesterification reaction at the temperature of 35-55 DEG C based on an ionic liquid as a solvent and vinyl ester fatty acid with C2-C18 carbon chain length as an acyl group donor and synthesizing to obtain the esterified derivative of lily polysaccharide. The method has the advantages that reaction condition is moderate and environment-friendly, the reaction is controllable and simple in process, the product is easy to separate from a reaction mixing system, and the like.

The invention discloses a preparation method of a water electrolysis oxygen evolution non-noble metal catalyst. The preparation method includes the steps that firstly, pyridine monomers I containing acyl or pyridine monomers I containing amidogen are added into a solvent, then monomers II containing amidogen or monomers II containing acyl and a catalyst are added in, and synthesis is performed by rising temperature; secondly, metal salt is added in, metal ions are added in for complexing, wherein according to the molar weight of the metal ions, the molar ratio of the metal ions to the pyridine monomers I containing acyl or the pyridine monomers I containing amidogen is 1-2: 1-2; thirdly, the solvent is removed, and the remaining obtained solid substances are dried for 8-24 hours at 80-100 DEG C; fourthly, mixed gas is introduced for heating, and primary heat treatment is performed; and fifthly, aftertreatment then is performed after temperature lowering, and the product is obtained. Active metal atoms of the non-noble metal catalyst prepared through the preparation method are evenly dispersed in a catalyst material, no metal-metal bonds exist, the metal utilizing rate reaches up to 100%, and the non-noble metal catalyst has the beneficial effects of being good in electric conduction performance, high in specific surface area, few in surface defect and the like.

The cross-linked hydrosilylation reaction product of an alkenyl functional silicone compound, a silylhydride functional silicone compound, and one or more allyl started, hydrogen, alkyl, aryl or acyl terminated polyether compounds exhibits stability, compatibility with polar organic solvents and is useful as a component in personal care compositions.

The invention discloses a new method for preparing cytidine. The method adopts the acyl-protected carbohydrate and acyl-protected cytosine as reactants and the acid or meta-acid ionic liquid as a catalyst, and comprises the following steps of: reacting at a temperature of (-5)-55 DEG C in a solvent for 5-20 hours to obtain a corresponding acyl-protected cytidine derivative; and saponifying to remove the protecting group to obtain cytidine. The new method disclosed by the invention has the advantages that: the catalyst has a wide source and is easily available; and the reaction conditions are mild, the operation is convenient, the yield is relatively high, the pollution is little, and the method can be applied to large-scale production.

The invention discloses a new method of preparing vilazodone intermediate 5-piperazin-2-acyl substituted benzofuran. The method comprises a coupling reaction of 5-halogen substituted 2-acyl substituted benzofuran (III) and piperazine compound (IV) in the presence of a metal palladium catalyst, a ligand, a solvent and a base to obtain the 5-piperazin-2-acyl substituted benzofuran. The method has advantages of short route, convenient synthesis and high yield, and is suitable for industrial production.