反应详情

To a solution of N-(2-aminoethyl)-2-(3-methoxyphenyl)pyrrolidine (0.58 g) in acetonitrile (15 ml) was added milled potassium carbonate (1.10 g) followed by 4-chlorobenzoyl chloride (0.33 ml) at ambient temperature, under nitrogen. The reaction mixture was stirred for 1.5 hrs, diluted with dichloromethane, and filtered. The filter cake was washed with dichloromethane, and the combined filtrates were concentrated. The residue was purified by flash column chromatography (silica gel, 0-20% methanol/dichloromethane). The appropriate fractions were collected and concentrated to afford 0.80 g (85%) of product. Trituration with ether/petroleum ether gave the analytical sample, mp 96°-98° C.

1. filtrationfiltered
2. washThe filter cake was washed with dichloromethane
3. concentrationthe combined filtrates were concentrated
4. customThe residue was purified by flash column chromatography (silica gel, 0-20% methanol/dichloromethane)
5. customThe appropriate fractions were collected
6. concentrationconcentrated