Copper promoted N-alkylation of sulfoximines with alkylboronic acid under mild conditions

Abstract

The copper meditated N-methylation of sulfoximines using methylboronic acid is reported. The reactions provide excellent yields in a short span of time under mild conditions. The optimized conditions were also found to be suitable for the N-alkylation of sulfoximine with different alkylboronic acids. In addition, N-methylation and cyclopropylation of the bioactive L-methionine sulfoximine derivative was demonstrated under standard reaction conditions.