Improvements of C–H Radio-Iodination of N-Acylsulfonamides toward Implementation in Clinics

Published as part of the Special Topic Halogenation methods (with a view towards radioimaging applications)

Abstract

An improved protocol to perform C–H radio-iodination is described. These new conditions allow rapid and clean formation of radio-iodinated N-acylsulfonamides using [¹²⁵I]NIS and catalytic amounts of palladium acetate and para-toluenesulfonic acid. No pre-functionalized precursors are required and the products are obtained with radiochemical conversions (RCC) of 27–84%.

Key words

radiochemistry - iodination - C–H activation - palladium - iodine­-125

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