US 12,269,790 B1
Process for the preparation of 2,4,6-triiodophenol derivatives
Zsolt Baranyai, Trieste (IT); Nicol Guidolin, Trieste (IT); Federica Lazzari, Novara (IT); and Fulvio Uggeri, Codogno (IT)
Assigned to BRACCO IMAGING S.P.A., Milan (IT)
Appl. No. 18/860,494
Filed by BRACCO IMAGING S.P.A., Milan (IT)
PCT Filed Apr. 28, 2023, PCT No. PCT/EP2023/061272
§ 371(c)(1), (2) Date Oct. 25, 2024,
PCT Pub. No. WO2023/209165, PCT Pub. Date Nov. 2, 2023.
Claims priority of application No. 22170765 (EP), filed on Apr. 29, 2022.
Int. Cl. C07C 235/48 (2006.01)
CPC C07C 235/48 (2013.01) 20 Claims
 
1. A process for the preparation of a 2,4,6-triiodophenol of formula (II), or a salt thereof,

OG Complex Work Unit Chemistry
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

OG Complex Work Unit Chemistry
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).