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filingDate 2001-11-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_45742d61186ca0708197f41446948cd5
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_74a73a8e588571f96da8f5008d76d6aa
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publicationDate 2004-11-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber NZ-526188-A
titleOfInvention A process for the preparation of iopamidol and the new intermediates therein
abstract A process for the preparation of (S)-N,N'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide of formula (I) (iopamidol) starting from 5-amino-N,N'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) is disclosed, wherein the process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein R1 is a hydrogen atom, a C1-C4 straight or branched alkoxy group, R2 is hydrogen, a C1-C4 straight or branched alkoxy group and R3 is a C1-C4 straight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic protections of the hydroxy groups in the carboxamido substituents under acidic conditions, when R is a group of formula A carboxamido hydroxy groups under acidic conditions. The formulae referred herein are as shown in the specification.
priorityDate 2000-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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