反应详情

A mixture of (S)-(+)-α-aminocyclohexanepropionic acid hydrate (5.00 g; 29.2 mmol) and phthalic dicarboxaldehyde (4.21 g; 31.3 mmol) in acetonitrile (120 mL) was refluxed for 20 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 (50 mL) to give 6.54 g (78%) of (S)-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 287.1521.

1. temperaturewas refluxed for 20 h under nitrogen
2. temperaturefurther cooled to 0° C
3. filtrationThe solid was filtered off
4. washwashed once with cold acetonitrile (50 mL)