- Preparation method of iopromide
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The invention belongs to the technical field of chemical synthesis, and particularly relates to a preparation method of iopromide. The method comprises the following steps: (1) chloridizing 5-methylaminoisophthalic acid monomethyl ester as shown in a formula II and used as a raw material to obtain 3-amino-5-chloroformylbenzoate as shown in a formula III; (2) enabling reaction between the compoundas shown in the formula III and methoxyacetyl chloride to obtain 3-chloroformyl 5-[methoxyacetyl)amino)]-methyl benzoate as shown in a formula IV; (3) enabling reaction between the compound as shown in the formula IV and 3-aminopropanediol to obtain 3-[(2,3-dihydroxypropylaminoformyl)-5-[(methoxyacetyl)amino]-methyl benzoate as shown in a formula V; (4) enabling reaction between the compound as shown in the formula V and 3-methylamino propanediol to obtain N,N'-di(2,3-dihydroxyl)-5-[(methoxyacetyl)amino)]-N-methyl-1,3-phthalamide as shown in a formula VI; and (5) enabling reaction between thecompound as shown in the formula VI and NaICl2 to obtain the iopromide. The preparation method of the iopromide provided by the invention is low in production cost, high in reproducibility and high inyield.
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- Preparation method of Iopromide and application of an intermediate thereof
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The invention relates to the field of iopromide. In order to solve the technical problems of the prior art that methods of preparing Iopromide are high purification difficulty, has complex steps and causes environmental pollution, the invention provides a preparation method of Iopromide and application of its intermediate; the preparation method comprises the steps of a, protecting by methoxy acetic anhydride, to be specific, a compound of formula (10) is allowed to react with methoxy acetic anhydride to obtain a compound of formula (II); b, allowing the compound of formula (10) to react with 3-methylamino-1,2-propanediol, hydrolyzing the product, and purifying to obtain Iopromide at a compound of formula (12); c, allowing the compound of step (12) to react with an iodization reagent to obtain iopromide of step (1); application of iopromide prepared via the compound of formula (10), (11) or (12) is also provided. The preparation method of iopromide has decreased environmental pollution and short reaction time, save energy and decrease energy composition; the post-treatment is simple, so that the cost is saved and the reaction is more environmentally efficiency and lower in cost.
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Paragraph 0057; 0061; 0065; 0069; 0074; 0079; 0084; 0089; 00
(2017/10/28)
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