http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105705483-A

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filingDate 2014-11-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ad1726b310bdcf96a81a95823b618796
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publicationDate 2016-06-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-105705483-A
titleOfInvention The preparation method of iopamidol
abstract The invention discloses a preparation method of iopamidol of formula (II) and comprising the following steps: a) compound (I) (wherein X is OR 2 or R 3 , and wherein R 2 and R 3 are C 1 -C 6 linear or branched alkyl, C 3 -C 6 ring Alkyl, C aryl, optionally substituted by a group selected from the group consisting of methyl, ethyl, n - propyl, i-propyl, n-butyl, sec-butyl, tert-butyl and phenyl) and The acylating agent (S)-2-(acetyloxy)propionyl chloride is reacted in a reaction medium to obtain an acetyloxy derivative of compound (I); b) by adding water or a dilute alkaline solution, such as hydrogen Sodium oxide or potassium hydroxide is used to hydrolyze the intermediate of step a) with an aqueous solution at a pH of 0 to 7, and the hydroxyl group is freed from the boron-containing protecting group to obtain the N-(S)-2-(acetyl group of compound (II) oxy)propionyl derivatives; c) base hydrolysis to restore the (S)-2-(hydroxy)propionyl group and give iopamidol (II), optionally recovering the boron derivative from the solution obtained in step b) thing. The boron-containing protecting groups are versatile, efficient and recyclable. A one-pot synthesis without the isolation of intermediates is provided, resulting in reduced recovered and recycled solvents and significantly increased yields, representing significant advantages in terms of cost-effectiveness and environmental awareness of the overall process.
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priorityDate 2013-11-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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