Process for the preparation of triiodinated carboxylic aromatic derivatives

摘要

The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available α-hydroxyacid or a salt thereof.

主权项

1. A process for the preparation of a compound of formulawhich process comprises reacting a compound of formula (II)with a α-hydroxyacid of formula (III)or a salt thereof, in the presence of a base,wherein:
R′ is hydrogen or a straight or branched C1-C6 alkyl group optionally substituted by one or more protected hydroxy groups; R is, the same in each occurrence, selected from the group consisting of alkoxy (—OR1), amino (—NH2 or —NHR1) and a chlorine atom; R1 is a straight or branched C1-C6 alkyl group optionally substituted by one or more protected hydroxy groups.