Application of micellar catalysis for a greener synthesis of Iopamidol

One of the most problematic steps in iodinated contrast agents synthesis (dx.doi.org/10.1021/cr200358s), is the amidation reaction: currently performed in aprotic dipolar solvents (DMF, NMP, DMAc). These solvents are subjected to an increasing regulatory pressure due to safety and environmental concerns. Our innovative protocol enables the amidation reaction between the acyl chloride intermediate and lipophilized serinol in water, the green solvent for excellence, by employing micellar catalysis technology (doi.org/10.1021/acs.oprd.0c00303), avoiding the use of such toxic solvents altogether.