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US 12,269,790 B1Granted
Process for the preparation of 2,4,6-triiodophenol derivatives
AssigneeBracco Imaging S.P.A.
InventorsZsolt Baranyai, Nicol Guidolin, Federica Lazzari, Fulvio Uggeri
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Abstract
The invention relates to a process for the preparation of a 2,4,6-triiodo-phenol derivative of formula (II), which is useful as an intermediate for the synthesis of conventional X-ray contrast agents, said process comprising the tri-iodination of the correspondent phenol derivative of said 2,4,6-triiodo-phenol derivative by means of an iodinating system comprising I2 and an oxide or a salt of an element of group 11 of the periodic table.
Claims20
A process for the preparation of a 2,4,6-triiodophenol of formula (II), or a salt thereof,
- wherein R and R′ represent, independently from one another, a moiety selected from the group consisting of hydrogen, —COOR1, and —CONR1R2;
- wherein R1 and R2 represent, independently from one another, hydrogen or a C1-C6 alkyl group optionally substituted by one or more groups selected from hydroxyl (—OH), C1-C6 alkoxy, and C1-C6 hydroxyalkoxy;
- comprising the following steps:
- a) providing a phenol of formula (I), or a salt thereof
- wherein R and R′ have the same meaning provided above;
- b) providing an iodinating system comprising I2, and at least an oxide or a salt of an element of group 11 of the periodic table, provided that when the element of group 11 is copper, the iodinating system further comprises phosphoric acid, carbonic acid, and/or ions thereof,
- c) reacting said phenol of step a) and said iodinating system of step b) in an aqueous medium having a pH comprised in the range of 7.0 to 9.0, to obtain the 2,4,6-triiodophenol of formula (II).
4 more elements
Dependencies are inferred from the claim text.