O-(Tetrahydropyran-2-yl)hydroxylamine → 2-methanesulfonyl-2-methyl-N-(tetrahydro-pyran-2-yloxy)-4-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-butyramide

Participants

Reaction Steps

The title compound (3.69 g, 60.4%) was prepared from (+/−)-2-methyl-2-(methylsulfonyl)-4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]butanoic acid (4.86 g, 12.7 mmol) and O-tetrahydro-2H-pyran-2-yl-hydroxylamine (2.1 g, 18.0 mmol) by a procedure analogous to that described for (+/−)-4-(4-bromophenyl)-2-methyl-2-(methylsulfonyl)-N-(tetrahydro-2H-pyran-2-yloxy)butanamide (III/Step 4—Preparation Number 2). LCMS m/z 480.3 (M−1).

Provenance & Evidence