Bracco Imaging S.p.a.

Camilla Cavallotti

Giovanni Battista Giovenzana

Luciano Lattuada

Fulvio Uggeri

Silvio Aime

Luisella Calabi

Giovanni Palmisano

Massimo Sisti

Rolf E Swenson

Pierfrancesco Morosini

Ramalingam Kondareddiar

Alessandro Minguzzi

Alberto Vertova

Letizia Sorti

Carlo Morelli

Ivan Menegotto

The invention is related to a process for preparing a iodinating X-rays contrast agent. More specifically, it relates to a process for the preparation of N,N'-bis-(2,3-dihydroxypropyl)-5-hydroxy-2,4,6-triiodo-1,3-benzenedicarboxaniide (I) by electrochemical iodination of N,N′-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide (II) with molecular iodine (I2) which is in situ electrochemically generated from a source of iodide ions (I−). The iodide ions (I−) are obtained by the dissolution of hydrogen iodide (HI) or an alkali metal iodide in the reaction medium or produced during the reaction of N,N′-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide with I2. The invention also relates to the use of the intermediate compound of formula (I), obtained through the above electrochemical iodination of compound (II), in the preparation of N,N′-bis[2,3-dihydroxypropyl]-5(hydroxyacetyl)methylamino]-2,4,6-triiodo-1,3-benzenedicarboxamide (iomeprol).

Electrochemical iodination of N,N'-(2,3-dihydroxypropyl)-5-hydroxy-1,3-benzenedicarboxamide

The present invention relates to a process for the preparation of iodinated phenols, &#x2014;in particular, it relates to a process including the electrochemical iodination of 3,5-disubstituted phenols of formula (1) to the corresponding 3,5-disubstituted-2, 4,6-triiodophenols of formula (2), which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves. Furthermore, the present invention includes the electrochemical iodination of 3, 5- disubstituted anilines of formula (6) to the corresponding 3,5-disubstituted-2,4,6-triiodoanilins of formula (7). 

Process for the iodination of aromatic compounds

Compounds of general formula (I): with substituents as defined herein and their chelates with bi-trivalent ions of the metal elements of atomic numbers 20 to 31, 39, 42, 43, 44, 49, and 57 to 83, and radioisotopes chosen amongPb,Ga,Ga,As,In,In,Y,Ru,Cu,Cu,Fe,Mn,La,Yb,Sm,Ho,Pm,Lu,Pr,Gd,Bi,Sc,Pm,Cu,Ag,Au,Tb,Cr,Tm,Ce,Yb,Y,Dy,Dy,Ru,Ru,Re,Tc,Bi,Bi,Bi,Rh,Pd,Sn,Sn andAu, as well as the salts thereof with physiologically compatible bases or acids.

Multidentate AZA ligands able to complex metal ions and the use thereof in diagnostics and therapy

Compounds of general formula (I): in which: Ris hydrogen, C&#x2013;Calkyl, C&#x2013;Ccycloalkyl, C&#x2013;Ccycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C&#x2013;Calkylene group or an ortho disubstituted arylene; Ris hydrogen, C&#x2013;Calkyl, C&#x2013;Ccycloalkyl, C&#x2013;Ccycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R, Rand Rare hydrogen, C&#x2013;Calkyl, C&#x2013;Ccycloalkyl, C&#x2013;Ccycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen amongPbGaGaAsInInYRuCuCuFeMnLaYbSmHoPmLuPrGdBiScPmCu,Ag,Au,Tb andCr as well as the salts thereof with physiologically compatible bases or acids 

Multidentate aza ligands able to complex metal ions and the use thereof in diagnostics and therapy

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Milan, Italy

Camilla Cavallotti