Reaktion #587439

Reaktionsgleichung

N,N-Diisopropylethylamine

(4-bromo-2-fluorophenyl)(hydroxy)acetic acid

methylamine

benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate

→

desired product

2-(4-bromo-2-fluorophenyl)-2-hydroxy-N-methylacetamide

Lösungsmittel

methylene chloride

Reaktionsbedingungen

Aufarbeitung

1. 1
   EinengenThe reaction mixture was concentrated
2. 2
   SonstigeThe residue was purified by chromatography on silica gel with 10% methanol in dichloromethane

Vorschrift

N,N-Diisopropylethylamine (0.2 mL, 0.001 mol) was added to a mixture of (4-bromo-2-fluorophenyl)(hydroxy)acetic acid (0.1 g, 0.4 mmol), methylamine (2M in THF, 0.24 mL, 0.48 mmol) and benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (0.21 g, 0.00048 mol) in methylene chloride (2 mL). The mixture was stirred at RT for 2 h. The reaction mixture was concentrated. The residue was purified by chromatography on silica gel with 10% methanol in dichloromethane to afford the desired product. LCMS: (M+H)=261.9/263.9.

Quelle