636 results about "Transmethylation" patented technology

A pharmaceutical composition useful as a preventive or therapeutic agent for immune-related diseases. The pharmaceutical composition includes at least HMG-COA reductase inhibitor and at least one amino alcohol compound having the following formula (I), a pharmacologically acceptable salt thereof, or a pharmacologically acceptable ester thereof

wherein R¹ and R² each represents hydrogen; R³ represents lower alkyl or hydroxymethyl; R⁴ represents hydrogen, alkyl, alkoxy or halogen; R⁵ represents hydrogen, halogeno, cyclohexyl or phenyl; X represents vinylene (CH═CH), oxygen, sulfur or methylated nitrogen; Y represents a single bond, oxygen, sulfur or carbonyl; Z represents a single bond or C₁-C₈ alkylene; n is 2 or 3.

Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 2-, 4-, or 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of using, synthesizing and manufacturing these analogs and derivatives are also provided. These compounds can be formulated into pharmaceutical compositions that can be used for treating any disease associated with aberrant DNA methylation, or a disease or condition that is sensitive to the treatment with decitabine or azacitidine, such as hematological disorders, tumors and cancers.

The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.

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.

Methods are disclosed for producing C₈ aromatic hydrocarbons. Representative methods comprise (a) fractionating an aromatic hydrocarbon containing feed stream (e.g., a feed stream comprising C₉ and/or C₁₀ aromatic hydrocarbons), to provide at least one methylated aromatic hydrocarbon-enriched fraction; and (b) reacting at least a portion of the at least one methylated aromatic hydrocarbon-enriched fraction in a transalkylation reaction zone to provide a transalkylation effluent comprising the C₈ aromatic hydrocarbons. The presence of a methylated aromatic hydrocarbon-enriched fraction in the inlet stream to the transalkylation reaction zone provides a number of advantages as described herein.

Enantiomers of S-adenosyl-l-methionine, their stable salts and their uses are described. These compositions possess potent activity in treating various conditions involving hypomethylation and transulfuration reactions and are valuable for use as active constituents in pharmaceutical compositions.

The invention provides a method for synthesizing methoxyamine hydrochloride and includes the following steps: ethyl acetate and hydroxylamine hydrochloride are added into a reaction vessel and 10 to 30 percent of sodium hydroxide solution is instilled for oximation reaction; then dimethyl sulfate is instilled, and at the same time sodium hydroxide solution with the mass fractions of 10 to 30 percent is instilled for methylation reaction; cold water is added after the temperature is decreased and a halohydrocarbon solvent is adopted for extraction; pressure is reduced under the temperature of 30 to 50 DEG C to recover the halohydrocarbon solvent and the product obtained is added into inorganic acid solution for hydrolysis reaction; after the hydrolysis is over, hydrochloride is used to obtain the product methoxyamine hydrochloride. The synthetic method which is simple improves the operation environment and increases the yield ratio.

The invention relates to the field of medicinal chemistry and pharmacotherapeutics and provides a 2-substituted arylethenyl-N-methylated quinoline derivative, a synthesis method thereof and an application of the 2-substituted arylethenyl-N-methylated quinoline derivative to the preparation of a drug for treating Alzheimer disease. The 2-substituted arylethenyl-N-methylated quinoline derivative has the chemical formula shown in the specification, wherein R1 in the formula is hydrogen, methylpiperazine, piperidine, morpholine, ethoxylpiperazine, dimethylaminoethylpiperazine or dimethylaminopropylpiperazine; R2 is para-substituted chlorine, fluorine, hydroxyl, methoxyl, dimethylamino, diethylin, methylpiperazine and morpholine, or ortho-substituted hydroxyl and methoxyl or meta-substituted methoxyl and nitro; R4 is hydrogen, chlorine, fluorine, hydroxyl, methoxyl, dimethylamino, diethylin, methylpiperazine or morpholine; R2 and R6 are hydrogen, hydroxyl or methoxyl; R3 and R5 are hydrogen, methoxyl or nitro. Experiments prove that the 2-substituted arylethenyl-N-methylated quinoline derivative provided by the invention has anticholinesterase activity, anti-Abeta aggregation and antioxidant activity.

The invention relates to a synthetic method of 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid, which belongs to the synthetic methods of heterocyclic compounds containing 1,3-thiazole ring. The synthetic method is characterized by comprising the following operation steps: 1) homogeneous oximation reaction: preparing 2-hydroxamic ethyl acetoacetate; 2) methylation reaction: preparing 2-methoxyimino ethyl acetoacetate; 3) triphosgene chlorination reaction: preparing 4-chloro-2-methoxyimino ethyl acetoacetate; 4) cyclization reaction: preparing 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid ethyl ester; 5) hydrolysis: preparing a crude product of the 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid; and 6) refining: preparing a product of the 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid. The invention provides an oximating agent system which is applicable to homogeneous nitrosification reaction. The invention provides a triphosgene chlorinating agent which has the advantages of small toxicity, safe and convenient storage, transportation and use, easy control of process operation and high yield. The yield of the 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid ethyl ester is not less than 95.4%; the yield of the crude product of the 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid is not less than 94.4%; and the yield of the finished product of the 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid is not less than 90.5%. The purity of the finished product of the 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyimino acetic acid is not less than 99.06%, and the melting point is 182.1 DEG C-183.9 DEG C. The synthetic method is used for synthesizing raw materials of the third generation of cephalosporins.

The invention discloses a novel method for synthesizing a 1,2,3-thiadiazole-5-formamidine compound. The target compound shown in general formula TDCA is prepared from a compound as shown in general formula M by virtue of a methylation reaction. The target component as shown in the general formula M is prepared from a compound as shown in general formula A and a compound as shown in general formula N by virtue of a condensation reaction, wherein during the methylation reaction, preferably, a catalyst is an organic metallic catalyst consisting of cuprous iodide and a ligand, namely 2,2,6,6-tetramethyl-3,5-heptadione; during the reaction, preferably, dimethylbenzene is taken as a solvent, and the optimum reaction temperature is 100-140 DEG C. The method disclosed by the invention is high in yield and more environment-friendly (as shown in Specification).

The invention discloses a method for preparing epsilon-caprolactone. After cyclohexanone, co-oxidation agents, catalysts, radical initiators and solvents are mixed, reaction is performed in air atmosphere, the co-oxidation agents are methylbenzene compounds, the catalysts are at least one of nitrates or oxides of Co, Fe and Cu, the solvents are at least one selected from 1, 2-dichloroethane, ethyl acetate and acetonitrile, and the method for preparing the caprolactone further co-produces aromatic aldehyde and aromatic acid. The method for preparing the epsilon-caprolactone takes aromatic methyl compounds as the co-oxidation agents, benzaldehyde is replaced, production cost is remarkably reduced, industrial production of the epsilon-caprolactone prepared by an oxygen/air oxidation method is possible, and the aromatic aldehyde and the aromatic acid are further co-produced when the epsilon-caprolactone is prepared by the method, so that the method had higher values in industrial application.

The invention discloses a novel synthesizing method of dapoxetine, wherein a series of reactions are carried out on trans-cinnamaldehyde and N-carbobenzoxy hydroxylamine which serve as initiative raw materials under the action of a self-prepared catalyst (s)-alpha-alpha-diisopropyl dimethyl tert-butyl silicon oxygroup prolinol, so that an important intermediate of the dapoxetine, namely an important chiral intermediate (S)-3-amino-3-phenyl propyl alcohol (compound 4), is obtained. The invention further discloses a preparation method of capecitabine, wherein the compound serving as a raw material is methylated and protected by hydroxyl and then reacts with 1-naphthol to form a salt, so that the capecitabine is obtained. The preparation method is easy in raw material obtainment, good in stereoselectivity and high in yield, thereby being suitable for industrial production.

The invention relates to methods for preparing and using laminine and pharmaceutically acceptable salts thereof. L-lysine is used an initiative material, and the method comprises the following steps of: protecting alpha-amino groups and carboxyl with metallic salts under an alkaline condition to form a chelate complex; performing separation and purification to obtain the chelate complex with the purity of 99 to 100 percent, and performing methylation on the chelate complex on epsilon-amino groups under the action of a phase transfer catalyst with a methylating agent to generate trimethyl lysine salts; removing metallic ions with a precipitator or chelating agent to obtain crude laminine and crude pharmaceutically acceptable salts thereof; and re-crystallizing the crude laminine and the crude pharmaceutically acceptable salts thereof with a solvent to obtain the medicinal laminine and the pharmaceutically acceptable salts thereof. The methylation of the separated and purified L-lysine metallic ion chelate complex and the phase transfer catalyst are simultaneously adopted, so the method remarkably reduces the generation of monomethyl substances, dimethyl substances and other byproducts, improves the yield and achieves the product purity of over 98.5 percent (HPLC).

There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.