Generating Monofluoro‐Substituted Amines and Amino Acids by the Interaction of Inexpensive KF and Sulfamidates.

The regioselective ring‐opening of 1,2‐ and 1,3‐sulfamidates with fluorine anion is reported. Direct construction of monofluoro‐substituted amines and amino acid derivatives using inexpensive and easily available potassium fluoride (KF). The monofluorination process only needs 35 minutes under heating, which will be an attractive route for the synthesis of the PET fluorine‐18 radiotracer. The application of the product can be extended to the construction of fluorinated polypeptides after simple deprotection treatment. [ABSTRACT FROM AUTHOR]