Abstract
We developed a versatile, rapid, and robust high‐yielding radiochemistry‐adapted protocol utilizing formamides as masking groups for secondary and tertiary amines. Selective reducing conditions were devised using borane reagents. In this protocol formamide functionalities were found to have an orthogonal reactivity to most other carbonyl functions, while effectively protecting amines from oxidative degradation. We exemplify the newly developed methodology by synthesizing a µ‐opioid PET radiotracer and a phenethylamine PET radiotracer analogue.
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