30 results about "Aminomalonic acid" patented technology

The present invention provides a processes, having practical utility, for preparing 2-oxindoles, N-hydroxy-2-oxindoles, or mixtures thereof comprising: catalytically hydrogenating a 2-nitroarylmalonate diester to produce a 2-(N-hydroxyamino)arylmalonate diester, a 2-aminoarylmalonate diester, or mixtures thereof as a first reaction intermediate; cyclizing, by intramolecular aminolysis of one ester group, the first reaction intermediate to produce a N-hydroxy-2-oxindole-3-carboxylate ester, 2-oxindole-3-carboxylate ester, or mixtures thereof as a second reaction intermediate; and hydrolyzing and decarboxylating the remaining ester group of the second reaction intermediate to produce the N-hydroxy-2-oxindole, the 2-oxindole, or mixtures thereof, wherein the cyclization reaction and the hydrolysis and decarboxylation reaction are conducted in situ with the catalytic hydrogenation reaction without isolation of said reaction intermediates.

The invention discloses a synthesis method of a pharmaceutical intermediate of tertiary butyl-(2-(biphenyl-4-yl)-1-(methylol) ethyl) carbamate, which comprises the steps that: diethyl acetamidornalonate and 4-substituent biphenyl are taken as initial raw materials and undergone six steps of reactions including condensation, decarboxylation, hydrolysis, reduction and acylation to obtain the tertiary butyl-(2-(biphenyl-4-yl)-1-(methylol) ethyl) carbamate. The method of the invention has the advantages of available raw materials, convenient operation, high reaction yield rate, recoverable solvents used in the synthesis course, thereby reducing environmental pollution and greatly reducing production cost; according to test results, the products obtained by the method has reliable quality and stable performance.

A composition comprising an amphoteric or pseudo-amphoteric agent and a polyhydroxy alpha hydroxyacid existing as a free acid, lactone, or salt, and isomeric or non-isomeric forms thereof is provided. The amphoteric or pseudo-amphoteric agent can be selected from amino acids, dipeptides, aminoaldonic acid, aminouronic acid, lauryl aminoproplyglycine, aminoaldaric acid, neuraminic acid desulfated heparin, deacetylated hyaluronic acid, hyalobiuronic acid, chondrosine, deacetylated chondroitin, creatine, creatinine, hydroxyproline, homocysteine, homocystine, homoserine, ornithine, citrulline, phosphatidylserine, and sphingomyelin. The composition may contain other additives, including cosmetic or pharmaceutical agents for topical treatment of dermatological disorders.

The invention relates to the technical field of medicine synthesis, and in particular, relates to a synthesis process of favipiravir and an intermediate thereof. The synthesis method of favipiravir comprises the following steps: 1) 2-aminopropanediamide and glyoxal serve as raw materials, and generating a compound III through a cyclization reaction; 2) performing benzyl protection on the compoundIII under the catalysis of potassium carbonate to generate a compound IV; 3) performing fluorine substitution on the compound IV under the action of fluorine gas, a solvent and a catalyst to generatea compound V; and 4) performing debenzylation protection on the compound V to generate favipiravir. Compared with other synthetic routes of favipiravir, the synthetic route provided by the invention has the advantages that the whole process route is shortened by virtue of high-selectivity fluorination reaction, the production cost is greatly reduced, and the synthesis process is suitable for industrial production.

The invention discloses a method for synthesizing an optically active intermediate N-tert-butoxycarbonyl-2-amino-8-nonenoic dicyclohexylamine salt. The method includes: taking acetamino malonate as an original raw material, performing alkylation reaction, hydrolysis and decarboxylation to generate an intermediate IV, subjecting the intermediate IV to tert-butoxycarbonyl protection to obtain an intermediate III, hydrolyzing the intermediate III under the action of enzymes to obtain an intermediate II, and allowing salt forming reaction between the intermediate II and dicyclohexylamine to obtain the target product. The method has the advantages of short synthetic route, easiness in purification of the synthesized product, mild reaction conditions and environment friendliness; the required raw material is cheap and low in cost; the obtained product is high in yield and quality and suitable for mass industrial production.

The invention relates to a chelate compound of amino malonic ester O, O'-Pt and N, O-Pt and a method for preparing the chelate compound almost purified.

The invention discloses a preparation method and intermediate of an isoquinoline compound. The isoquinoline compound is roxadustat, the intermediate of the roxadustat is a compound formula 2, and twonovel preparation methods of a roxadustat key intermediate 9 are developed by taking the compound formula 2 as a raw material. According to the first method, a compound 2 reacts with hydroxylamine hydrochloride to obtain an intermediate compound formula 3, and then the intermediate compound formula 3 reacts with a phosphine reagent compound formula 4 to obtain the roxadustat key intermediate compound formula 9. According to the second method, acyl chloride is prepared from the compound formula 2, then the acyl chloride and an aminomalonate ester derivative 7 are subjected to condensation and decarboxylation reaction, then a compound formula 8 is obtained, and finally, the key intermediate compound formula 9 is obtained. The two methods are high in yield, using of precious metal for catalysis is avoided, the route efficiency is greatly improved, the technological cost is lowered, generation of by products is reduced, and the purity of final finished products is improved advantageously;and a route is easy to operate, the total yield is high, the purity of obtained products is also high, the route is suitable for amplifying production, and the route is shows as the formula (please see the specifications for the formula).

The invention discloses a synthetic method of a monoamino inhibitor intermediate monoethyl 2-acetylamino-2-benzylmalonate. The method comprises the following steps: 1, carrying out amino protection on a compound I diethyl aminomalonate and di-tert-butyl dicarbonate to obtain a compound II diethyl-2-Boc-aminomalonic acid; 2, reacting the compound II with benzyl bromide to obtain a compound III diethyl 2-(N-(tertbutyloxycarbonyl)amino)-2-benzylmalonate; 3, removing monoester from the compound III to obtain a compound IV monoethyl 2-(N-(tertbutyloxycarbonylamino)-2-benzyl-malonate; 4, carrying out amino deprotection on the compound IV to obtain a compound V monoethyl 2-amino-2-benzyl-malonate; and 5, carrying out an acetylation reaction on the compound V to prepare a compound VI monoethyl 2-(N-acetylamino)-2-benzyl-malonate. The method has the advantages of simple reactions, easily available raw materials, simple post-treatment, high yield, low cost, high operationality, and suitableness for industrial production.

The invention relates to 2-(2-methacrylamide triglycyl) aminomalonate ester (I) with a structural formula as below as well as a preparation method and application thereof. The 2-(2-methacrylamide triglycyl) aminomalonate ester (I) can be applied to preparing an aminomalonate platinum complex Prolindac; the preparation method has short synthesis steps, simple and convenient operation, good product quality, high yield and easy industrialized production; and wherein R is equal to (C1 to C5) alkyl.

The invention relates to a preparation method of chemicals, in particular to a preparation method of 2-aminomalonamide. The invention provides a synthesis method of 2-aminomalonamide, which comprises the following steps: dropwise adding a solution of diethyl 2-aminomalonate hydrochloride into ammonia water, and controlling the reaction temperature to be below 10 DEG C; and after the reaction is finished, crystallizing to obtain a solid, namely the 2-aminomalonamide. The synthesis method is short in production period and beneficial to reduction of production cost; only two steps of dropwise adding and devitrifying are needed, so that the operation is simple; and only one reaction container is needed in the whole process, and the reaction container does not need to be replaced in the process, so that the production efficiency is improved. The purity of the prepared 2-aminomalonamide is up to 99.5% or above, and the yield of the 2-aminomalonic acid diethyl ester hydrochloride is up to 99.0% or above.

The present invention provides a novel thermosensitive cyclotriphosphazene-platinum complex conjugates represented by Formula (1) wherein m is a repeating unit of poly(alkoxyethylene glycol) selected from the integers 2, 7 and 12; n represents the length of the alkyl chain selected from the integers 0, 1, 2 and 3; x represents the length of the anionic amino acid residue selected from the integers 0 (amino malonic acid derivatives), 1 (aspartic acid derivatives) and 2 (glutamic acid derivatives); A2 is a bidentate chelating diamine selected from the group consisting of 2,2-dimethyl-1,3-propanediamine (dmpda), trans(+/-)-1,2-diaminocyclohexane (dach) and 1,1-diaminomethylcyclohexane (dmach).

The invention discloses a preparation method of aminomalonic acid diethyl ester hydrochloride, which comprises the following steps: 1, carrying out nitrosation on malonic acid diethyl ester in acetic acid by using a nitrous acid aqueous solution to obtain oximido malonic acid diethyl ester; 2, carrying out catalytic hydrogenation reaction on the oximido diethyl malonate in an alcohol solvent by using a nickel-containing three-way catalyst to obtain aminodiethyl malonate; 3, filtering out the catalyst from the hydrogenated liquid, salifying the compound by using hydrogen chloride ethanol under cooling, desolventizing the solution, and crystallizing the liquid by using acetone to obtain the diethyl aminomalonate hydrochloride. The method has the characteristics of milder and safer reaction conditions, simplicity and convenience in operation, high yield, low cost, good quality and the like, and has a wide application prospect. In addition, according to the hydrogenation technology used in the method, waste residues, waste acid and the like generated by reduction of zinc powder are avoided, and the defects that a palladium-carbon catalyst is high in price and prone to poisoning and inactivation are overcome.

The invention provides an efficient synthesis method of weight-reducing component tartronic acid in cucumbers, which comprises the following steps: S1, preparing tartronic acid: carrying out diazotization reaction on aminomalonic acid serving as a raw material to obtain tartronic acid; S2, carrying out diazotization reaction on aminomalonic acid and sodium nitrite in a dilute acid; S3, after diazotization reaction is finished, directly heating and hydrolyzing without separation, and then concentrating under reduced pressure to obtain a solid; S4, adding an alcohol to remove salt, and recovering the alcohol to obtain a tartronic acid crude product; and S5, dissolving the tartronic acid crude product with an acid, filtering, decolorizing, and recovering the acid to obtain tartronic acid . The method has the advantages that aminomalonic acid with wide sources is used as the raw material, and the tartronic acid is obtained in one step through diazotization reaction, so that the problem ofraw material sources is solved, and the defects of high raw material cost, complex product, difficulty in separation and purification and the like are overcome; the method has the advantages of easily available raw materials, high raw material conversion rate, high purity and yield, stable process conditions and simple operation.

A modulator of metabolic processes and method of manufacturing same is provided. The invention may have applicability in at least the fields of medicine, veterinary medicine, medical industry, and agriculture. The essence of invention is a chemically modified biopolymer with a polypeptide chain as an exogenous modulator of metabolic and energy exchange processes between a cell and environment, characterized in that it comprises chlorine atoms covalent-bonded with nitrogen atoms of polypeptide chain to the amount of 0.5 to 40% of the total mass of modified biopolymer, whereas the polypeptide chain includes methionine sulfoxide, cysteinic, α-aminomalonic and α-aminoacetoacetic acids to the amount of 1-20 acid residues per 1 mole of final product. The proposed modulator possesses large resource of free energy due to high degree of oxidation, thus ensuring catalytic activity when interacting with clue enzymes and return of particular organs and systems to normal physiological condition.