Ethyl bromoacetate → (1,3-Dioxo-1,3-dihydro-isoindol-2-ylamino)-acetic acid ethyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-amino-isoindole-1,3-dione (5.0 g, 30.9 mmol), ethyl bromoacetate (10.32 g, 61.8 mmol), K2CO3 (8.5 g, 61.8 mmol) in DMA (38 ml) was heated at 80° C. for 7 h. After cooling to rt, the mixture was filtered, and the filtrate was diluted with EtOAc, washed with water and brine, dried and concentrated. The residue was treated with EtOAc and hexanes to give 393A (4.4 g, 57%) as yellow crystals.

Provenance & Evidence