6-methoxy-2,4-dihydro-1H-3,1-benzoxazine-2,4-dione → 4-(2,4-Dimethoxy-benzyl)-7-methoxy-3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione

Participants

Reaction Conditions

Reaction Steps

6-Methoxy-2H-3,1-benzoxazine-2,4(1H)-dione (23 g, 119 mmol) and (2,4-dimethoxy-benzylamino)-acetic acid 1 (27 g, 120 mmol) were suspended in p-xylene (500 mL) and heated under argon at reflux (140° C.) for 2 h. The hot solution was allowed to cool to rt, while spontaneous crystallization occurred. The crystals were filtered off and washed with p-xylene (50 mL). Yield: 39 g (92%). mp 196° C. m/z 356 (M).

Provenance & Evidence