We report the formation of iminium-trifluoroborates (TIMs) from potassium acyltrifluoroborates (KATs) and the synthesis of α-aminotrifluoroborates and α-aminoboronic acids from TIMs.
Oxidative amidation of potassium acyltrifluoroborates (KATs) and amines via trifluoroborate iminiums (TIMs) delivers amides without coupling agents. This unusual approach to amides can be applied for the late-stage modification of bioactive molecules and for solid-phase peptide synthesis.
Except for insufficient FFP dosing per patient and limitations on assessment of indications for prescribing, transfusion practices were in agreement with national guidelines.
The cross-coupling of α-aminoalkyltrifluoroborates and Grignard reagents to form N, N-substituted α-tertiary amines (ATAs) is reported. Key to the success of this reaction is the unexpected oxidation of the α-aminoalkyltrifluoroborate to the corresponding iminium cation by commercially available Barluenga's reagent. Various Grignard reagents added smoothly, enabling the synthesis of a variety of ATAs, which are of high value for medicinal chemistry and drug development. Many of the reported examples are not accessible by the established methods.
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