- Method for preparing iopromide intermediate
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The invention discloses a method for preparing an iopromide intermediate. The method comprises the following steps: 1) taking a compound I5-amino-2,4,6-triiodo-1,3-benzoyl chloride and methoxyacetyl chloride as raw materials, triethylamine as an acidifyin
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Paragraph 0038-0040; 0043-0044; 0046-0047; 0049-0059
(2019/09/17)
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- The new method of preparing [...] (by machine translation)
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The invention relates to a preparation method of iopromide. 5-methoxylacetamido-2,4,6-triiodo m-phthalic acid[(2-oxo-1,3-dioxolame-4-yl)methyl]amido chloride (Formula V) and 5-methoxylacetamido-2,4,6-triiodo m-phthalic acid{[(2-oxo-1,3-dioxolame-4-yl)methyl]-(2,3-dyhydroxyl-N-methyl propyl)}diamide (Formula VI) are introduced to be used as intermediates. Even if there is no additional purification step, a bismer by-product generated during the reaction also can be removed by introduction of the intermediates and high-purity iopromide can be prepared at high yield.
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Paragraph 0035; 0036
(2018/12/13)
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- A method for preparing [...]
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The present invention relates to an X-ray contrast agent iopromide preparation method. According to the method, 3-methoxy acetyl-5-(2,3-dihydroxy-N-methyl-n-propyl-carbamoyl)-2,4,6-triiodobenzoic acid (4) is introduced as an intermediate, the used raw material is cheap and easy to obtain, the experiment operation is relatively simple, the reaction condition is mild, and the product purity is qualified.
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Paragraph 0025; 0035; 0036
(2018/12/13)
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- The new method of preparing [...]
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The present invention relates to iopromide preparation methods, and provides three new iopromide preparation methods, wherein the method 1 comprises that a compound represented by a formula II is adopted as a starting raw material and reacts with allylamine to obtain a compound represented by a formula III, the compound represented by the formula III reacts with N-methyl allylamine to obtain a compound represented by a formula IV, the compound represented by the formula IV reacts with methoxyacetyl chloride to obtain a compound represented by a formula V, and the compound represented by the formula V is oxidized to obtain the iopromide represented by a formula I, the method 2 comprises that the compound represented by the formula II is adopted as a starting raw material and reacts with allylamine to obtain the compound represented by the formula III, the compound represented by the formula III reacts with methoxyacetyl chloride to obtain a compound represented by a formula IV-1, the compound represented by the formula IV-1 reacts with N-methyl allylamine to obtain the compound represented by the formula V, and the compound represented by the formula V is oxidized to obtain the iopromide represented by the formula I, the method 3 comprises that the compound represented by the formula II is adopted as a starting raw material and reacts with allylamine to obtain the compound represented by the formula III, the compound represented by the formula III reacts with methoxyacetyl chloride to obtain the compound represented by the formula IV-1, the compound represented by the formula IV-1 reacts with 3-methylamino-1,2-propanediol to obtain a compound represented by a formula V-1, and the compound represented by the formula V-1 is oxidized to obtain the iopromide represented by the formula I, and the method 4 comprises that the compound represented by the formula II is adopted as a starting raw material and reacts with methoxyacetyl chloride obtain a compound represented by a formula III-1, the compound represented by the formula III-1 reacts with allylamine to obtain the compound represented by the formula IV-1, the compound represented by the formula IV-1 reacts with N-methyl allylamine to obtain the compound represented by the formula V, and the compound represented by the formula V is oxidized to obtain the iopromide represented by the formula I.
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Paragraph 0045; 0046
(2018/12/13)
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- A new method for synthesizing iodine proletariat amine
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The invention discloses a novel synthesis method for iopromide. The novel synthesis method comprises the following steps of 1, enabling methoxyacetic acid to react with triphosgene to obtain a reaction product, and then, enabling the reaction production to be directly subjected to one-pot reaction with 5-amino-2, 4, 6-triiodo-isophthalicacyl chloride to prepare a compound 5-[(2-methoxyl) acetamido]-2, 4, 6-triiodo-isophthalicacyl chloride as shown in the formula (II); 2, condensing the compound as shown in the formula (II) and N-methyl-2, 3-dihydroxyl propylamine under the action of a solid catalyst ZrO2-Cr2O3 to obtain a compound 5-[(2-methoxyl) acetamido]-3-(2, 3-dihydroxyl-N-methylpropylaminoformoxyl)-2, 4, 6-triiodo-benzoyl chloride as shown in the formula (III); 3, condensing the compound as shown in the formula (III) and 2, 3-dihydroxylpropylamine under the action of a catalyst to prepare a compound iopromide as shown in the formula (I). The synthesis method for iopromide, disclosed by the invention, is few in byproduct, easy to control the product quality, high in product purity, cheap and easily-obtained in used reagent, few in step, simple in operation, relatively high in total yield and suitable for industrial production, and provides a novel approach for preparing iopromide.
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Paragraph 0025; 0026
(2018/02/03)
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- A METHOD FOR PREPARING AN INTERMEDIATE OF IOPROMIDE
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The present invention relates to a method for preparing an intermediate of iopromide, and more particularly, to a method for preparing an intermediate of iopromide, in which 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid dichloride is produced using 1,4-dioxane as a reaction solvent, and then reacted with 3-amino-1,2-propanediol using a solvent mixture of 1,4-dioxane or tetrahydrofuran (THF) and isopropanol as a reaction solvent to obtain the intermediate of iopromide with a faster reaction time, a smaller amount of solvent, and a higher yield.
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Paragraph 118-121
(2015/05/06)
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- NOVEL PROCESS FOR PREPARATION OF IOPROMIDE
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The present invention relates to a novel process for preparing iopromide which is used as a contrast agent for X-ray, wherein 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid (2,3-diacetoxypropyl)amide chloride of formula (19) and 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-diacetoxypropyl)]diamide of formula (20) are introduced as intermediates, by which a bismer by-product generated during the preparation process can be removed even without an additional removal procedure and thus iopromide with high purity can be prepared in high yield.
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Page/Page column 6
(2011/02/26)
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- NOVEL PROCESS FOR PREPARATION OF IOPROMIDE
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The present invention relates to a novel process for preparing iopromide which is used as a contrast agent for X-ray, wherein 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid (2,3-diacetoxypropyl)amide chloride of formula (19) and 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-diacetoxypropyl)]diamide of formula (20) are introduced as intermediates, by which a bismer by-product generated during the preparation process can be removed even without an additional removal procedure and thus iopromide with high purity can be prepared in high yield.
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Page/Page column 10-11
(2009/12/05)
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- Nonionic X-ray contrast agents, compositions and methods
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Triiodinated isophthalamide derivatives, useful as X-ray contrast agents, having at least one amide group derived from the amino-alcohol, 3-(N-2-hydroxyethyl)amino-1,2-propanediol, which provides high water solubility and low mammalian toxicity, and methods of preparing them. Methods of preparing 3-(N-2-hydroxyethyl)amino-1,2-propanediol are provided.
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- Novel triiodinated isophthalic acid diamides as nonionic X-ray contrast media
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New triiodinated isophthalic acid diamides of the formula STR1 wherein the amide residues --CO--N.R1 R2 and --CO--N.R3 R4 are different from each other and R1 is hydrogen or C1-6 alkyl, R2 is mono- or polyhydroxyalkyl, R3 is hydrogen or C1-6 alkyl, R4 is mono- or polyhydroxylalkyl, R5 is C1-6 alkyl or mono- or polyhydroxy-C1-6 -alkyl or C1-3 -alkoxy-C1-3 -alkyl, and R6 is hydrogen, C1-6 alkyl or mono- or polyhydroxyalkyl provide superior nonionic X-ray contrast media.
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