Rapid Iododeboronation with and without Gold Catalysis: Application to Radiolabelling of Arenes.

摘要: Radiopharmaceuticals that incorporate radioactive iodine in combination with single-photon emission computed tomography imaging play a key role nuclear medicine, applications drug development and disease diagnosis. Despite this importance, there are relatively few general methods for the incorporation of radioiodine into small molecules. This work reports rapid air- moisture-stable ipso-iododeboronation procedure uses NIS non-toxic, green solvent dimethyl carbonate. The fast reaction mild conditions gold-catalysed method led to highly efficient process radiolabelling arenes, which constitutes first example an application homogenous gold catalysis selective radiosynthesis. was exemplified by synthesis radiolabelled meta-[125 I]iodobenzylguanidine, radiopharmaceutical is used therapy human norepinephrine transporter-expressing tumours.