反应详情

A mixture of (R)-(+)-α-aminocyclohexanepropionic acid hydrochloride (2.69 g; 15.7 mmol) and phthalic dicarboxaldehyde (2.50 g; 14.6 mmol) in acetonitrile (60 mL) was refluxed for 42 h under nitrogen. The mixture was allowed to cool to room temperature and further cooled to 0° C. The solid was filtered off and washed once with cold acetonitrile to give 2.65 g (63%) of (R)-3-Cyclohexyl-2-(1-oxo-1,3-dihydro-isoindol-2-yl)-propionic acid as a white solid: EI-HRMS m/e calcd for C17H21NO3 (M+) 287.1521, found 287.1523.

1. temperaturewas refluxed for 42 h under nitrogen
2. temperaturefurther cooled to 0° C
3. filtrationThe solid was filtered off
4. washwashed once with cold acetonitrile