反应详情

Add benzyl (R,R)-2-methylcyclopropanecarboxylate (0.55 g, 2.89 mmol) to a 0° C. solution of 3-(3-fluoro-4-methoxyphenyl)isothiazol-5-ylamine (0.59 g, 2.63 mmol) and trimethylaluminum (2.0 M in toluene, 5.26 mmol) in dichloromethane (5 mL) and allow reaction to naturally warm to room temperature. Warm the reaction mixture to 40° C. and allow to stir overnight. Dilute the reaction mixture with EtOAc (100 mL) and 1 N HCl (40 mL) and water (100 mL), collect the organic phase, and evaporate. Chromatography over silica gel eluting with 25-50% EtOAc in hexane affords (R,R)—N-[3-(3-fluoro-4-methoxyphenyl)isothiazol-5-yl]-2-methylcyclopropane-carboxamide. Yield: 55.9%. ES-MS: m/e 307.0 (m+1).

1. customreaction
2. temperatureWarm the reaction mixture to 40° C.
3. customcollect the organic phase
4. customevaporate