C07C237/46

Process for the Preparation of Intermediates Useful in the Preparation of Non-ionic Contrast Agents

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

Process for the Preparation of Intermediates Useful in the Preparation of Non-ionic Contrast Agents

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

Process for the Preparation of Intermediates Useful in the Preparation of Non-ionic Contrast Agents

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

IODINATED COMPOUNDS HAVING RADIOCONTRAST PROPERTIES

The present disclosure pertains to iodinated compounds that comprise at least one 2,4,6-triiodobenzene moiety in which at least one of the hydrogens at 1-, 3- and 5-positions of the 2,4,6-triiodobenzene moiety is substituted by an iodinated substituent that comprises one or more iodophenyl-containing groups. The present disclosure also pertains to compositions containing such iodinated compounds and methods of making such iodinated compounds.

IODINATED COMPOUNDS HAVING RADIOCONTRAST PROPERTIES

The present disclosure pertains to iodinated compounds that comprise at least one 2,4,6-triiodobenzene moiety in which at least one of the hydrogens at 1-, 3- and 5-positions of the 2,4,6-triiodobenzene moiety is substituted by an iodinated substituent that comprises one or more iodophenyl-containing groups. The present disclosure also pertains to compositions containing such iodinated compounds and methods of making such iodinated compounds.

Process for the preparation of iopamidol

The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a Ci-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness. ##STR00001##

Process for the preparation of iopamidol

The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a Ci-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness. ##STR00001##

Purification of X-ray contrast agents

The present invention relates to a process for purification of iodinated X-ray contrast agents and in particular to purification of crude dimeric contrast agents, such as Iodixanol and Ioforminol. More particularly, the invention relates to purification of such X-ray contrast agents using membrane technology to remove monomeric impurities.

Purification of X-ray contrast agents

The present invention relates to a process for purification of iodinated X-ray contrast agents and in particular to purification of crude dimeric contrast agents, such as Iodixanol and Ioforminol. More particularly, the invention relates to purification of such X-ray contrast agents using membrane technology to remove monomeric impurities.

Purification of X-ray contrast agents

The present invention relates to a process for purification of iodinated X-ray contrast agents and in particular to purification of crude dimeric contrast agents, such as Iodixanol and Ioforminol. More particularly, the invention relates to purification of such X-ray contrast agents using membrane technology to remove monomeric impurities.